An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors

Article Biochemistry & Molecular Biology

Discovery of dual tubulin-NEDDylation inhibitors with antiproliferative activity

Dong-Jun Fu et al.

Summary: In this study, a series of potential dual tubulin-NEDDylation inhibitors were synthesized and evaluated. Compound C11 exhibited the strongest antiproliferative activity and showed potent inhibition against tubulin and NEDDylation.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

添加到收藏夹

Article Oncology

Cancer statistics, 2022

Rebecca L. Siegel et al.

Summary: Each year, the American Cancer Society compiles data on cancer occurrence and outcomes in the United States. The latest data shows that breast and prostate cancer progress has stagnated, while lung cancer has shown improvements in survival rates. Lung cancer incidence for advanced disease has declined while localized-stage rates have increased, resulting in higher survival rates. Mortality patterns align with incidence trends, with lung cancer deaths declining rapidly, breast cancer deaths slowing, and prostate cancer deaths stabilizing.

CA-A CANCER JOURNAL FOR CLINICIANS (2022)

添加到收藏夹

Review Biochemistry & Molecular Biology

Recent Advances in Combretastatin A-4 Inspired Inhibitors of Tubulin Polymerization: An Update

Sultan Nacak Baytas

Summary: Cancer, a leading cause of fatality worldwide, is being extensively researched for therapeutic strategies. Advances in molecular sciences and high throughput techniques have identified microtubules as attractive targets for cancer therapy. The development of new microtubule-targeting agents, particularly analogues of combretastatin A-4, has been a focus of research since 2015.

CURRENT MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Identification and optimization of biphenyl derivatives as novel tubulin inhibitors targeting colchicine-binding site overcoming multidrug resistance

Bao Cheng et al.

Summary: In this study, a novel compound dxy-1-175 with potent anticancer activity was discovered by modifying the structure of the compound. It was found to inhibit cancer cell proliferation by interacting with tubulin and was able to overcome multidrug resistance. The improved compound 12e showed superior inhibitory effects on tumor growth in vivo.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities

Ya-Xin Sun et al.

Summary: This study designed a series of novel bis-substituted aromatic amide dithiocarbamate derivatives as tubulin inhibitors with potential anticancer activities. Among them, compound 20q exhibited the most potent antiproliferative activity and was identified as a tubulin inhibitor targeting the colchicine binding site.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Multidisciplinary

Design, synthesis and biological evaluation of novel 2-phenyl-4,5,6,7-tetrahydro-1H-indole derivatives as potential anticancer agents and tubulin polymerization inhibitors

Guangcheng Wang et al.

Summary: A series of new 2-phenyl-4,5,6,7-tetrahydro-1H-indole derivatives were synthesized and evaluated for their anti-proliferative activities, with one compound showing the most potent anticancer activity against breast cancer and lung cancer cells while sparing normal liver cells. Mechanism studies revealed that the compound arrested cell cycle and induced apoptosis, and effectively inhibited tubulin polymerization with an inhibitory mechanism similar to colchicine. Molecular docking studies indicated high binding affinities for the colchicine binding pocket of tubulin, suggesting potential as new tubulin polymerization inhibitors.

ARABIAN JOURNAL OF CHEMISTRY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors

Zhan Wang et al.

Summary: A series of new colchicine glycoconjugates were designed as tubulin polymerization inhibitors and their antiproliferative activities were evaluated. Among them, compound 1e exhibited excellent selectivity and low cytotoxicity. Moreover, it significantly inhibited tubulin polymerization and disrupted microtubule networks.

BIOORGANIC & MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis, biological assessment, and in-Silico studies of 1,2,4-triazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors

Heba S. Mohamed et al.

Summary: A series of 1,2,4-triazolo[1,5-alpha]pyrimidine derivatives were designed and synthesized as combretastatin CA-4 analogs. Among them, compound 4c showed significant anticancer and tubulin polymerization inhibition activities, presenting a promising lead compound for further development.

BIOORGANIC CHEMISTRY (2022)

添加到收藏夹

Article Pharmacology & Pharmacy

IMB5476, a novel microtubule inhibitor, induces mitotic catastrophe and overcomes multidrug resistance in tumors

Yan-Bo Zheng et al.

Summary: IMB5476, a novel nitrobenzoate microtubule inhibitor, exhibits increased aqueous solubility. It disrupts microtubule networks in cells, causing cell cycle arrest and inducing cell death through mitotic catastrophe and apoptosis. IMB5476 also inhibits angiogenesis and overcomes multidrug resistance.

EUROPEAN JOURNAL OF PHARMACOLOGY (2022)

添加到收藏夹

Article Chemistry, Medicinal

SAR of Novel 3-Arylisoquinolinones: meta-Substitution on the Aryl Ring Dramatically Enhances Antiproliferative Activity through Binding to Microtubules

Mai A. Elhemely et al.

Summary: A set of meta-substituted 3-arylisoquinolinones with substantial cytotoxicity in various cancer cell lines has been discovered. These compounds have the potential to mimic colchicine and interact with microtubules, leading to antiproliferative effects and inhibition of endothelial cell formation.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Physical

Design and synthesis of novel substituted indole-acrylamide derivatives and evaluation of their anti-cancer activity as potential tubulin-targeting agents

Mohammed Hawash et al.

Summary: In this study, novel compounds with polar and nonpolar substitutions on the prop-2-en-1-on linker of the trans-indol-3-ylacrylamide scaffold were designed and synthesized. The antiproliferative activities of these compounds against hepatocellular carcinoma were evaluated, and five of the compounds showed moderate antitumor activities. Compound 13 was identified as a tubulin polymerization inhibitor and induced G2/M-phase arrest in Huh7 cells. The results suggest that polar substitutions enhance the potency against tubulin polymerization.

JOURNAL OF MOLECULAR STRUCTURE (2022)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site

Xiang-Yu Yan et al.

Summary: A series of novel diphenylamine derivatives were synthesized and evaluated for their anti-proliferative activities against human cancer cell lines. Among them, compound 5f exhibited promising anti-proliferative activity against HT29 cells and showed inhibitory effects on cancer cell migration, colony formation, and angiogenesis. Further studies revealed that compound 5f inhibited tubulin polymerization, arrested HT29 cell cycle, induced cell apoptosis, and inhibited tumor growth in animal models. The compound also demonstrated good pharmacokinetic properties. These findings suggest that compound 5f has potential as an antitumor candidate and warrants further investigation.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects

Huajian Zhu et al.

Summary: A series of novel multifunctional vascular disrupting agents (VDAs) was designed and synthesized, among which compound TH-6 showed the most potent antiproliferative activity against a panel of cancer cell lines. TH-6 inhibited tubulin assembly and increased the acetylation level of HDAC substrate proteins, leading to effective tumor growth inhibition without apparent toxicity. Furthermore, TH-6 disrupted both the internal and peripheral tumor vasculatures, contributing to persistent tumor inhibitory effects. Therefore, TH-6 deserves further investigation for its potential as a new approach in clinical cancer therapy.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Review Biochemistry & Molecular Biology

Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy

Mohammed Hawash

Summary: Cancer is a leading cause of death globally, and despite advancements in discovering new anti-cancer candidates, it continues to result in numerous deaths. Tubulin protein, which plays a critical role in cell division and intracellular transportation, has become one of the main targets for anti-cancer agents. Inhibiting microtubule formation by targeting tubulin protein can induce cell death. Recent studies have focused on designing and synthesizing novel compounds that target tubulin and have demonstrated anticancer activity against various cancer cell lines. Tubulin inhibitors have shown promising results in inhibiting cancer cell viability, inducing apoptosis, and effectively binding with the colchicine binding site of tubulin.

BIOMOLECULES (2022)

添加到收藏夹

Article Engineering, Multidisciplinary

Anticancer Activity of Thiophene Carboxamide Derivatives as CA-4 Biomimetics: Synthesis, Biological Potency, 3D Spheroid Model, and Molecular Dynamics Simulation

Mohammed Hawash et al.

Summary: This study synthesized thiophene carboxamide derivatives as biomimetics of the anticancer medication Combretastatin A-4 (CA-4) and compared their similarity in polar surface area (PSA) to CA-4. The results showed that most of the synthesized structures had biomimetic PSA to CA-4 and exhibited similar chemical and biological properties against Hep3B cancer cell line. Compounds 2b and 2e in the synthesized series showed the highest activity against Hep3B, and they had comparable interaction patterns to CA-4 and colchicine within the tubulin-colchicine-binding pocket.

BIOMIMETICS (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and bioevaluation of 2,7-diaryl-pyrazolo[1,5-a]pyrimidines as tubulin polymerization inhibitors

Runlai Liu et al.

Summary: The newly designed compound 6d showed significant antiproliferative activity against MCF-7 cancer cells, inhibiting cancer cell growth and migration through multiple pathways.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation

Shannon Pecnard et al.

Summary: A series of cyclic bridged analogs of isocombretastatin A-4 with compound 42 showed high antiproliferative activity against a panel of cancer cell lines, as well as strong activity against colon-carcinoma cells and MDR1-overexpressing K562R cell line. Compound 42 also effectively inhibited tubulin polymerization, induced cell cycle arrest, and caused caspase-induced apoptosis in K562 cells. Additionally, compound 42 was significantly less cytotoxic in non-cancer cells compared to isoCA-4.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of indole-based [1,2,4] triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors

Cheng-Jun Wu et al.

Summary: A series of novel microtubulin polymerization inhibitors based on indole were designed and synthesized, among which compound 12d exhibited the highest antiproliferative activity by inducing cellular apoptosis, cell cycle arrest, and inhibiting tubulin polymerization.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of tanshinone IIA-based analogues: Potent inhibitors of microtubule formation and angiogenesis

He Huang et al.

Summary: The structural optimization of tanshinone IIA led to the discovery of a new analogue, 2f, with potent anti-cancer properties, including inhibition of tubulin assembly, induction of apoptotic cell death, and suppression of cell proliferation, migration, and invasion. Additionally, 2f exhibited promising in vivo anti-angiogenic effects.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Identification of new 3-phenyl-1H-indole-2-carbohydrazide derivatives and their structure-activity relationships as potent tubulin inhibitors and anticancer agents: A combined in silico, in vitro and synthetic study

Rungroj Saruengkhanphasit et al.

Summary: Utilizing three different virtual screening techniques, eight new derivatives of 3-phenyl-1H-indole-2-carbohydrazide with antiproliferative activities were identified; among them, 27a exhibited the most potent tubulin inhibitory activity and induced G2/M phase arrest. Derivatives 27b, 27d, and 27i showed strong activities against various cell lines, with bromine substitution at R1 position demonstrating the most prominent anticancer effects.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Structure-activity relationships and antiproliferative effects of 1,2,3,4-4H-quinoxaline derivatives as tubulin polymerization inhibitors

Tingting Liang et al.

Summary: Colchicine binding site inhibitors have great potential for treating tumors. Tetrahydro-quinoxaline derivatives designed in this study showed promising antitumor activities, with compound 11a being the most potent candidate.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Oncology

Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

Hyuna Sung et al.

Summary: The global cancer burden in 2020 saw an estimated 19.3 million new cancer cases and almost 10.0 million cancer deaths. Female breast cancer surpassed lung cancer as the most commonly diagnosed cancer, while lung cancer remained the leading cause of cancer death. These trends are expected to rise in 2040, with transitioning countries experiencing a larger increase compared to transitioned countries due to demographic changes and risk factors associated with globalization and a growing economy. Efforts to improve cancer prevention measures and provision of cancer care in transitioning countries will be crucial for global cancer control.

CA-A CANCER JOURNAL FOR CLINICIANS (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of novel indole-1,2,4-triazole derivatives as tubulin polymerization inhibitors

Meng-Ke Wu et al.

Summary: A series of novel indole-1,2,4-triazole derivatives were synthesized and evaluated for their potential as tubulin polymerization inhibitors, with compound 12 demonstrating significant anti-proliferative activity in vitro. It arrested cell cycle at the G2/M phase, induced apoptotic cell death, and showed possible interaction with tubulin heterodimers, suggesting potential for future cancer research.

DRUG DEVELOPMENT RESEARCH (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities

Huajian Zhu et al.

Summary: Novel N-benzylbenzamide derivatives 20b and its corresponding disodium phosphate 20b-P show significant anti-cancer activity with excellent safety profile, making them promising anti-tubulin agents for further investigation in cancer therapy.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Novel Benzimidazole and Indazole Analogues as Tubulin Polymerization Inhibitors with Potent Anticancer Activities

Yichang Ren et al.

Summary: Novel indazole and benzimidazole analogues, such as compound 12b, demonstrated potent antiproliferative activities against cancer cells, with IC50 values comparable to colchicine. Compound 12b also showed in vivo antitumor efficacy in a melanoma tumor model, suggesting its potential as a promising lead compound for further investigation as a potential anticancer agent.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities

Yichang Ren et al.

Summary: Compound 3b, designed as a tubulin inhibitor targeting the colchicine binding site, showed high antiproliferative activity against HepG-2 cells, with the ability to suppress microtubule polymerization, disrupt dynamics, inhibit cancer cell migration, induce cell cycle arrest and apoptosis. Docking studies indicated its potential as a novel tubulin inhibitor deserving further investigation.

BIOORGANIC & MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization

Shu-Yu Wang et al.

Summary: In this study, indoline derivatives were designed, synthesized, and found to exhibit potent antiproliferative activity against various cell lines, with compound 9d identified as a tubulin inhibitor targeting the colchicine binding site. Molecular docking results confirmed the tight binding of compound 9d to the tubulin site, indicating its potential as a novel tubulin inhibitor with anticancer activity.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Pyrazoline derivatives as tubulin polymerization inhibitors with one hit for Vascular Endothelial Growth Factor Receptor 2 inhibition

Bing Yang et al.

Summary: In this study, a series of pyrazoline derivatives bearing 3,4,5-trimethoxy phenyl and thiophene moieties were synthesized and evaluated as tubulin polymerization inhibitors. The top hit compound, 3q, showed potent anti-proliferation activity on cancer cell lines and comparable efficacy with less toxicity than the positive control Colchicine. Further investigations indicated the potential for improving tubulin polymerization inhibition and introducing VEGFR2 inhibition through ring transposition.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design and discovery of new antiproliferative 1,2,4-triazin-3(2H)-ones as tubulin polymerization inhibitors targeting colchicine binding site

Ibrahim H. Eissa et al.

Summary: Thirty-five new colchicine binding site inhibitors were designed and synthesized based on the 1,2,4-triazin3(2H)-one nucleus. Two compounds showed significant antiproliferative effects against three human cancer cell lines, and further investigation revealed their potential as tubulin polymerization inhibitors. The synthesized compounds demonstrated selectivity against cancer cells and upregulated levels of active caspase-3 and pro-apoptotic protein Bax, suggesting their potential as anti-cancer agents. Additionally, in silico studies showed promising interactions with the colchicine binding site and favorable pharmacokinetic properties.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines

Xian-Sen Huo et al.

Summary: The novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidine derivatives showed great potential as tubulin polymerization inhibitors, with high antiproliferative activity and selectivity against cancer cells. These compounds inhibit tumor cell growth by affecting the cell cycle, inducing apoptosis, and inhibiting tubulin polymerization.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of Stable Colchicine-Binding Site Tubulin Inhibitors 6-Aryl-2-benzoyl-pyridines as Potential Anticancer Agents

Hao Chen et al.

Summary: The study optimized the structure of a potent tubulin inhibitor, leading to the synthesis of analogues with improved metabolic stability. High-resolution X-ray crystal structures confirmed direct binding of two compounds to tubulin. In vitro and in vivo experiments demonstrated the efficacy of one compound, 60c, as a potential anticancer agent.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Novel Anti-Breast-Cancer Inhibitors by Synergistically Antagonizing Microtubule Polymerization and Aryl Hydrocarbon Receptor Expression

Kun Wang et al.

Summary: Compound 12, a novel dual-receptor inhibitor targeting both tubulin and AhR, showed strong anti-breast-cancer activity with potent inhibition of tumor growth in cell lines and xenograft models, as well as inducing apoptosis in breast cancer cells. Its ability to synergistically antagonize tubulin and AhR makes it a promising candidate for further development as an effective and safe anti-breast-cancer drug.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Recent Progress on Tubulin Inhibitors with Dual Targeting Capabilities for Cancer Therapy

Wen Shuai et al.

Summary: Microtubules are crucial in cellular functions and important targets for cancer therapy, but drug resistance and toxicity limit their efficacy. Dual-target drugs, combining tubulin with other anti-tumor agents, are considered promising to overcome limitations and improve therapeutic efficacy. Rational target combinations and design strategies of dual-target tubulin inhibitors are discussed for future directions.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of Novel Diarylamide N-Containing Heterocyclic Derivatives as New Tubulin Polymerization Inhibitors with Anti-Cancer Activity

Xu Liu et al.

Summary: Through the design and synthesis of a series of N-containing heterocyclic derivatives, a novel tubulin polymerization inhibitor with potential anti-tumor activity was identified, which could achieve its anti-cancer activity by inhibiting tubulin polymerization and disrupting microtubule networks.

MOLECULES (2021)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors

Peng-Cheng Diao et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of 1-(benzofuran-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazole derivatives as tubulin polymerization inhibitors

Zhi-Yuan Qi et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

A synthetic 2,3-diarylindole induces microtubule destabilization and G2/M cell cycle arrest in lung cancer cells

Bongkotrat Thanaussavadate et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design and synthesis of newer 1,3,4-oxadiazole and 1,2,4-triazole based Topsentin analogues as anti-proliferative agent targeting tubulin

Fatima Naaz et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of novel 5,6,7-trimethoxy-N-aryl-2-styrylquinolin-4-amines as potential anticancer agents and tubulin polymerization inhibitors

Salimeh Mirzaei et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

The discovery of novel indazole derivatives as tubulin colchicine site binding agents that displayed potent antitumor activity both in vitro and in vivo

Ying-Jie Cui et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

New thiazole-2(3H)-thiones containing 4-(3,4,5-trimethoxyphenyl) moiety as anticancer agents

Mahsa Ansari et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase

Shixian Hua et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site

Yu-Ying Shao et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties

Hao Chen et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of 2-alkoxycarbonyl-3-anilinoindoles as a new class of potent inhibitors of tubulin polymerization

Romeo Romagnoli et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of a novel tubulin inhibitor SKLB0565 targeting the colchicine binding site

Xi Hu et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and evaluation of antiproliferative and antitubulin activities of 5-methyl-4-aryl-3-(4-arylpiperazine-1-carbonyl)-4H-1,2,4-triazoles

Chao Wang et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Fluorinated derivatives of 2-phenyl-3-hydroxy-4(1H)-quinolinone as tubulin polymerization inhibitors

Jiri Rehulka et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents

Yonghua Liu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

1,4,5,6,7,8-Hexahydroquinolines and 5,6,7,8-tetrahydronaphthalenes: A new class of antitumor agents targeting the colchicine binding site of tubulin

Mennatallah A. Shaheen et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors

Wen Shuai et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility

Valery K. Brel et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities

Gang Li et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway

Jian Song et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a] pyridine analogues as new potent tubulin polymerization inhibitors

Fang Yang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin

JiaPeng He et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Synthesis, biological evaluation, and molecular docking analysis of phenstatin based indole linked chalcones as anticancer agents and tubulin polymerization inhibitors

Jyoti Kode et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study

Weifeng Ma et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors

Huajian Zhu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis, and anticancer evaluation of benzophenone derivatives bearing naphthalene moiety as novel tubulin polymerization inhibitors

Guangcheng Wang et al.

BIOORGANIC CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain

Wenlong Li et al.

BIOORGANIC CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site

Wenlong Li et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Synthesis, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site

Wenlong Li et al.

BIOORGANIC CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

N,N-bis-heteroaryl methylamines: Potent anti-mitotic and highly cytotoxic agents

Ilhem Khelifi et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain

Wei Zhao et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

1-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy

Junhang Jiang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis, Anticancer Activity and Molecular Modeling Studies of Novel Chalcone Derivatives Containing Indole and Naphthalene Moieties as Tubulin Polymerization Inhibitors

Guangcheng Wang et al.

CHEMICAL & PHARMACEUTICAL BULLETIN (2019)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents

Feijie Xu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop

Oskia Bueno et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Structure-Guided Design, Synthesis, and Biological Evaluation of (2-(1H-Indo1-3-yl)-1H-imidazol-4-yl)(3,4,5-trinnethoxyphenyl) Methanone (ABI-231) Analogues Targeting the Colchicine Binding Site in Tubulin

Qinghui Wang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis, and biological evaluation of 1-substituted-2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents

Ling Li et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of certain benzyl/phenethyl thiazolidinone-indole hybrids as potential anti-proliferative agents: Synthesis, molecular modeling and tubulin polymerization inhibition study

Dilep Kumar Sigalapalli et al.

BIOORGANIC CHEMISTRY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Novel [1,2,4]triazolo [1,5-a]pyrimidine derivatives as potent antitubulin agents: Design, multicomponent synthesis and antiproliferative activities

Fang Yang et al.

BIOORGANIC CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Discovery and optimization of 3,4,5-trimethoxyphenyl substituted triazolylthioacetamides as potent tubulin polymerization inhibitors

Fang Yang et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of flexible and rigid analogs of 4H-1,2,4-triazoles bearing 3,4,5-trimethoxyphenyl moiety as new antiproliferative agents

Mahsa Ansari et al.

BIOORGANIC CHEMISTRY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and biological evaluation of resveratrol-cinnamoyl derivates as tubulin polymerization inhibitors targeting the colchicine binding site

Yong Yin et al.

BIOORGANIC CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

3,5-Diaryl-1H-pyrazolo[3,4-b]pyridines as potent tubulin polymerization inhibitors: Rational design, synthesis and biological evaluation

Min'an Zhai et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis, biological evaluation, and molecular docking investigation of 3-amidoindoles as potent tubulin polymerization inhibitors

Peng Chen et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors

Dong-Jun Fu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study

Muhamad Mustafa et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity

Wenlong Li et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of pyrimidine bridged combretastatin derivatives as potential anticancer agents and mechanistic studies

Bhupinder Kumar et al.

BIOORGANIC CHEMISTRY (2018)

添加到收藏夹

Article Chemistry, Medicinal

New 6-and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors

Giuseppe La Regina et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

添加到收藏夹

Article Chemistry, Medicinal

Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site

Qinhuai Lai et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

添加到收藏夹

Review Cell Biology

Microtubule-Targeting Agents: Strategies To Hijack the Cytoskeleton

Michel O. Steinmetz et al.

TRENDS IN CELL BIOLOGY (2018)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Novel 4-Arylisochromenes as Anticancer Agents Inhibiting Tubulin Polymerization

Wenlong Li et al.

ACS MEDICINAL CHEMISTRY LETTERS (2018)

添加到收藏夹

Article Oncology

A Potent, Metabolically Stable Tubulin Inhibitor Targets the Colchicine Binding Site and Overcomes Taxane Resistance

Kinsie E. Arnst et al.

CANCER RESEARCH (2018)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis and biological evaluation of curcumin inspired indole analogues as tubulin polymerization inhibitors

P. V. Sri Ramya et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis of C5-tethered indolyl-3-glyoxylamide derivatives as tubulin polymerization inhibitors

Sravanthi Devi Guggilapu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis, antiproliferative, anti-tubulin activity, and docking study of new 1,2,4-triazoles as potential combretastatin analogues

Muhamad Mustafa et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

添加到收藏夹

Article Multidisciplinary Sciences

Design, synthesis and structure-activity relationship of 3,6-diaryl7H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazines as novel tubulin inhibitors

Qile Xu et al.

SCIENTIFIC REPORTS (2017)

添加到收藏夹

Article Biochemistry & Molecular Biology

New indole-based chalconoids as tubulin-targeting antiproliferative agentsd

Hassan Mirzaei et al.

BIOORGANIC CHEMISTRY (2017)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, Synthesis of Novel Platinum(II) Glycoconjugates, and Evaluation of Their Antitumor Effects

Jianbin Han et al.

CHEMICAL BIOLOGY & DRUG DESIGN (2016)

添加到收藏夹

Review Pharmacology & Pharmacy

Tubulin inhibitors in non-small cell lung cancer: looking back and forward

R. Ferrara et al.

EXPERT OPINION ON PHARMACOTHERAPY (2016)

添加到收藏夹

Article Chemistry, Medicinal

Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety

Vikas Chaudhary et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

添加到收藏夹

Review Cell Biology

Microtubules: 50 years on from the discovery of tubulin

Gary Borisy et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2016)

添加到收藏夹

Article Multidisciplinary Sciences

The γ-tubulin-specific inhibitor gatastatin reveals temporal requirements of microtubule nucleation during the cell cycle

Takumi Chinen et al.

NATURE COMMUNICATIONS (2015)

添加到收藏夹

Article Oncology

A phase I clinical trial assessing the safety and tolerability of combretastatin A4 phosphate injections

Peng Liu et al.

ANTI-CANCER DRUGS (2014)

添加到收藏夹

Article Chemistry, Multidisciplinary

Highly water-soluble platinum(II) complexes as GLUT substrates for targeted therapy: improved anticancer efficacy and transporter-mediated cytotoxic properties

Pengxing Liu et al.

CHEMICAL COMMUNICATIONS (2013)

添加到收藏夹

Review Chemistry, Multidisciplinary

Glucose conjugation for the specific targeting and treatment of cancer

Emilia C. Calvaresi et al.

CHEMICAL SCIENCE (2013)

添加到收藏夹

Article Oncology

Phase I Clinical and Pharmacokinetic Evaluation of the Vascular-Disrupting Agent OXi4503 in Patients with Advanced Solid Tumors

Dan M. Patterson et al.

CLINICAL CANCER RESEARCH (2012)

添加到收藏夹

Review Biochemistry & Molecular Biology

Tanshinones: Sources, Pharmacokinetics and Anti-Cancer Activities

Yong Zhang et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2012)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Microtubule-binding agents: a dynamic field of cancer therapeutics

Charles Dumontet et al.

NATURE REVIEWS DRUG DISCOVERY (2010)

添加到收藏夹

Article Oncology

A phase I study of ABT-751, an orally bioavailable tubulin inhibitor, administered daily for 21 days every 28 days in pediatric patients with solid tumors

Elizabeth Fox et al.

CLINICAL CANCER RESEARCH (2008)

添加到收藏夹

Article Chemistry, Medicinal

Targeting the Delivery of Glycan-Based Paclitaxel Prodrugs to Cancer Cells via Glucose Transporters

Yih-Shyan Lin et al.

JOURNAL OF MEDICINAL CHEMISTRY (2008)

添加到收藏夹

Article Oncology

Phase I dose-finding and pharmacokinetic trial of orally administered indibulin (D-24851) to patients with solid tumors

I. E. L. M. Kuppens et al.

INVESTIGATIONAL NEW DRUGS (2007)

添加到收藏夹

Review Oncology

Microtubules as a target for anticancer drugs

MA Jordan et al.

NATURE REVIEWS CANCER (2004)

添加到收藏夹

Article Multidisciplinary Sciences

Insight into tubulin regulation from a complex with colchicine and a stathmin-like domain

RBG Ravelli et al.

NATURE (2004)

添加到收藏夹

Review Multidisciplinary Sciences

Dynamics and mechanics of the microtubule plus end

J Howard et al.

NATURE (2003)

添加到收藏夹

Article Biochemistry & Molecular Biology

Mapping the binding site of colchicinoids on β-tubulin -: 2-chloroacetyl-2-demethylthiocolchicine covalently reacts predominantly with cysteine 239 and secondarily with cysteine 354

RL Bai et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2000)

添加到收藏夹

An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors

相关参考文献

导出引文

分享论文