☆ 4.6 Article

Design and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

相关参考文献

注意：仅列出部分参考文献，下载原文获取全部文献信息。

Article Biochemistry & Molecular Biology

Synthesis, molecular modelling and QSAR study of new N-phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with antiproliferative activity

Mona F. Said et al.

Summary: In this study, two new sulphonamide compounds were synthesised and tested for their inhibitory activity against multiple isoforms of carbonic anhydrase. Compound 2h showed the most effective inhibition against hCA I and hCA II, while compound 3c exhibited promising selectivity towards lung cancer cell line A549.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

The three-tails approach as a new strategy to improve selectivity of action of sulphonamide inhibitors against tumour-associated carbonic anhydrase IX and XII

Alessandro Bonardi et al.

Summary: Human carbonic anhydrase isoforms IX and XII have been confirmed as anticancer targets, with three-tails approach showing higher selectivity against tumor-associated isoforms and demonstrating anti-proliferative effects in various cancer cell lines. X-ray crystallography studies have been conducted to investigate the binding mode of these inhibitors, providing valuable insights for potential cancer treatments.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

4-Anilinoquinazoline-based benzenesulfonamides as nanomolar inhibitors of carbonic anhydrase isoforms I, II, IX, and XII: design, synthesis, in-vitro, and in-silico biological studies

Hossam Nada et al.

Summary: In this study, a series of 4-anilinoquinazoline-based benzenesulfonamides were designed and synthesized as potential carbonic anhydrase inhibitors (hCAIs). These compounds showed high inhibitory activity and have potential applications in the treatment of epilepsy, glaucoma, and cancer.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Oncology

Inhibition of carbonic anhydrases IX/XII by SLC-0111 boosts cisplatin effects in hampering head and neck squamous carcinoma cell growth and invasion

Annachiara Sarnella et al.

Summary: The study demonstrates that using the CA IX/XII specific inhibitor SLC-0111 can enhance the sensitivity of HNSCC to cisplatin, reducing proliferation, migration, and invasion of cells. Furthermore, combination therapy can inhibit the activation of cell signaling pathways such as STAT3, AKT, ERK, and EMT program, while inducing apoptosis in cancer cells.

JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH (2022)

添加到收藏夹

Article Chemistry, Medicinal

Development of 4-((3-oxo-3-phenylpropyl)amino)benzenesulfonamide derivatives utilizing tail/dual-tail approaches as novel carbonic anhydrase inhibitors

Mostafa M. Elbadawi et al.

Summary: In this study, tail/dual tail approaches were used to design and synthesize benzenesulfonamide derivatives as new SLC-0111 analogs with carbonic anhydrase (CA) inhibitory activity. The results showed that these derivatives had varying effects on different CA isoforms. Appending a second hydrophilic tail significantly enhanced the inhibitory activities towards hCA IX and hCA XII isoforms. SAR analysis revealed the importance of grafting the sulfamoyl functionality at para-position and incorporating a bulky hydrophobic tail for CA inhibitory activity. The most potent hCA IX inhibitors exhibited strong cell growth inhibitory activity against breast cancer cell lines.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Benzenesulfonamides with different rigidity-conferring linkers as carbonic anhydrase inhibitors: an insight into the antiproliferative effect on glioblastoma, pancreatic, and breast cancer cells

Francesco Liguori et al.

Summary: In this study, a new library of compounds incorporating a urea linker into an imidazolidin-2-one cycle was found to potently inhibit four different hCAs in the nanomolar range. These compounds exhibited promising anti-proliferative effects comparable to SLC-0111.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Immunology

The emerging role of 27-hydroxycholesterol in cancer development and progression: An update

Saade Abdalkareem Jasim et al.

Summary: Oxysterols are cholesterol metabolites with various biological functions, including their involvement in cancer development and immunological suppression. Specifically, 27-hydroxycholesterol (27-HC) may act as an estrogen and promote the growth of estrogen receptor (ER) positive breast cancer cells. However, the precise role of 27-HC in cancer promotion and progression is still debatable, and more research is needed to uncover the exact function of these molecules.

INTERNATIONAL IMMUNOPHARMACOLOGY (2022)

添加到收藏夹

Proceedings Paper Materials Science, Multidisciplinary

In-vitro evaluation of anticancer activity of natural flavonoids, apigenin and hesperidin

Sarmad Dheyaa Noori et al.

Summary: The primary goal of this study is to investigate the preventive impacts of bioactive natural flavonoids such as Apigenin and Hesperidins on different cancer models in vitro. The findings suggest that these flavonoids exhibit cytotoxic effects on various cancer cell lines and have potential anti-tumor properties.

MATERIALS TODAY-PROCEEDINGS (2022)

添加到收藏夹

Article Pharmacology & Pharmacy

Design, synthesis, molecular modeling, and biological evaluation of acrylamide derivatives as potent inhibitors of human dihydroorotate dehydrogenase for the treatment of rheumatoid arthritis

Fanxun Zeng et al.

Summary: Human DHODH is a promising target for cancer and autoimmune disease treatment. Novel DHODH inhibitors were designed and synthesized, with compound 11 identified as lead for SAR studies. Optimization efforts led to potent compounds with promising anti-arthritic effects in vivo.

ACTA PHARMACEUTICA SINICA B (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of a novel series of indolylchalcone-benzenesulfonamide hybrids acting as selective carbonic anhydrase II inhibitors

Priti Singh et al.

Summary: The study shows that the combination of primary sulfonamide and indolylchalcone can effectively design new compounds with good inhibitory activity against human carbonic anhydrase. These newly synthesized molecules exhibit varying levels of inhibition against different isoforms, with some compounds showing stronger activity against specific isoforms.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Exploring of tumor-associated carbonic anhydrase isoenzyme IX and XII inhibitory effects and cytotoxicities of the novel N-aryl-1-(4-sulfamoylphenyl)-5-(thiophen-2-yl)-1H-pyrazole-3-carboxamides

Cem Yamali et al.

Summary: A series of novel N-aryl-1-(4-sulfamoylphenyl)-5-(thiophen-2-yl)-1H-pyrazole-3-carboxamides were synthesized and evaluated as inhibitors of carbonic anhydrase isoforms. Some compounds showed selective inhibition towards cancer-related isoforms and moderate cytotoxicity against various cancer cell lines, indicating their potential as anticancer drug candidates.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Investigation of 3-sulfamoyl coumarins against cancer-related IX and XII isoforms of human carbonic anhydrase as well as cancer cells leads to the discovery of 2-oxo-2H-benzo[h]chromene-3-sulfonamide - A new caspase-activating proapoptotic agent

Dmitry Dar'in et al.

Summary: This study synthesized a set of novel coumarin sulfonamide derivatives, some of which showed potent antiproliferative activity against human carbonic anhydrase, especially exhibiting significant selective inhibition against A431 human epidermoid carcinoma cells. These findings suggest that compound 10q may serve as a promising lead compound for the development of new-generation anticancer agents.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

RCSB Protein Data Bank: powerful new tools for exploring 3D structures of biological macromolecules for basic and applied research and education in fundamental biology, biomedicine, biotechnology, bioengineering and energy sciences

Stephen K. Burley et al.

Summary: RCSB PDB, as the US data center for the global PDB archive, provides free access to 3D macromolecular structure data for millions of users worldwide, including educators, students, and the general public, integrating over 40 external biodata resources. The redesigned website now features improved search functionality and easier access to PDB data, showcasing new structures relevant to the understanding and addressing of the COVID-19 pandemic.

NUCLEIC ACIDS RESEARCH (2021)

添加到收藏夹

Article Chemistry, Medicinal

Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors

Ozlem Akgul et al.

Summary: A series of taurine substituted sulfonamide derivatives with ureido moiety at the tail section were synthesized as selective inhibitors of tumor associated human Carbonic Anhydrase (CA) IX and XII. These derivatives showed a strong dependence on the presence of ureido moiety and demonstrated highly stabilized ligand-protein complex with specific amino acid residues in both hCA II and hCA IX-mimic.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities

Mostafa M. Elbadawi et al.

Summary: New derivatives show enhanced inhibitory action against cancer-related CA IX isoform, indicating promising candidates for potential anticancer drugs, with further evaluation in breast and colon cancer cell lines.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Quinoline-sulfamoyl carbamates/sulfamide derivatives: Synthesis, cytotoxicity, carbonic anhydrase activity, and molecular modelling studies

Elmas Begum Cakmak et al.

Summary: Carbonic anhydrase (CA) IX and XII isoforms are highly expressed in various human tissues and cancers, with CA IX being a prominent target due to its overexpression in hypoxic tumors. A study synthesized and characterized twenty-seven novel compounds with inhibitory activities against CA I, CA II, CA IX, and CA XII isoforms, among which compound 2m showed the highest inhibition against hCA IX. Furthermore, compounds 3a, 3e, and 3f exhibited the most cytotoxic effects across different cell lines.

BIOORGANIC CHEMISTRY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Development of Novel Quinoline-Based Sulfonamides as Selective Cancer-Associated Carbonic Anhydrase Isoform IX Inhibitors

Moataz Shaldam et al.

Summary: A new series of quinoline-based benzenesulfonamides (QBS) have been developed as potential carbonic anhydrase inhibitors, with para-sulphonamide derivatives showing the best inhibitory activity. In addition, a linker elongation approach and molecular docking simulation studies were used to further investigate the anticancer effects of QBS.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis, in?vitro inhibition and toxicological evaluation of human carbonic anhydrases I, II and IX inhibitors in 5-nitroimidazole series

Ashok Aspatwar et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action

Alessandro Bonardi et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Chemistry, Medicinal

PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia

Justyna M. Gawel et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Discovery of new ureido benzenesulfonamides incorporating 1,3,5-triazine moieties as carbonic anhydrase I, II, IX and XII inhibitors

Nabih Lolak et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, synthesis and molecular docking of novel pyrazolo [1,5-a] [1,3,5] triazine derivatives as CDK2 inhibitors

Khulood H. Oudah et al.

BIOORGANIC CHEMISTRY (2019)

添加到收藏夹

Article Chemistry, Multidisciplinary

A magnetically recoverable copper-salen complex as a nano-catalytic system for amine protection via acetylation using thioacetic acid

Elahe Yazdani et al.

RESEARCH ON CHEMICAL INTERMEDIATES (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Inhibition studies on a panel of human carbonic anhydrases with N1-substituted secondary sulfonamides incorporating thiazolinone or imidazolone-indole tails

Fadi M. Awadallah et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2018)

添加到收藏夹

Article Biochemistry & Molecular Biology

Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies

Li Liu et al.

MEDCHEMCOMM (2018)

添加到收藏夹

Article Multidisciplinary Sciences

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

Antoine Daina et al.

SCIENTIFIC REPORTS (2017)

添加到收藏夹

Article Chemistry, Medicinal

A BOILED-Egg To Predict Gastrointestinal Absorption and Brain Penetration of Small Molecules

Antoine Daina et al.

CHEMMEDCHEM (2016)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis, carbonic anhydrase inhibition and cytotoxic activity of novel chromone-based sulfonamide derivatives

Fadi M. Awadallah et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2015)

添加到收藏夹

Article Chemistry, Medicinal

Synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives as 15-lipoxygenase inhibitors

Mohammad Mahdavi et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2014)

添加到收藏夹

Article Chemistry, Physical

Recyclable, highly efficient and low cost nano-MgO for amide synthesis under SFRC: A convenient and greener 'NOSE' approach

Vijay Kumar Das et al.

APPLIED CATALYSIS A-GENERAL (2013)

添加到收藏夹

Article Chemistry, Medicinal

Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors

Bo Song et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)

添加到收藏夹

Article Chemistry, Multidisciplinary

Nano rod-shaped and reusable basic Al2O3 catalyst for N-formylation of amines under solvent-free conditions: A novel, practical and convenient 'NOSE' approach

Vijay Kumar Das et al.

GREEN CHEMISTRY (2012)

添加到收藏夹

Article Crystallography

Spectroscopic Studies and Structure of 4-(3-Benzoylthioureido)benzoic Acid

Fatma Aydin et al.

JOURNAL OF CHEMICAL CRYSTALLOGRAPHY (2010)

添加到收藏夹

Article Chemistry, Medicinal

Model-Free Drug-Likeness from Fragments

Oleg Ursu et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2010)

添加到收藏夹

Article Chemistry, Multidisciplinary

Synthesis and Anti-inflammatory Activity of Some Novel 3-(6-Substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4 (3H)-ones

Manish Srivastav et al.

E-JOURNAL OF CHEMISTRY (2009)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

Claudiu T. Supuran

NATURE REVIEWS DRUG DISCOVERY (2008)

添加到收藏夹

Review Chemistry, Medicinal

Carbonic Anhydrases as drug targets - An overview

Claudiu T. Supuran

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2007)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.