Quantitative Structure-Activity Relationship Evaluation of MDA-MB-231 Cell Anti-Proliferative Leads

Article Chemistry, Medicinal

Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?

Gerasimos Rassias et al.

Summary: This study identified a novel B2 receptor agonist with significant antiproliferative activity in breast cancer cells, which may be achieved through multiple mechanisms, providing new insights for the development of anticancer drugs.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Discovery of a novel small-molecule inhibitor of Fam20C that induces apoptosis and inhibits migration in triple negative breast cancer

Rongyan Zhao et al.

Summary: A new small-molecule inhibitor, 3r, of Fam20C was obtained through combining in silico high-throughput screening with chemical synthesis methods, which exhibited desired antiproliferative activities against MDA-MB-231 cells and also inhibited migration. This inhibitor was found to induce apoptosis via the mitochondrial pathway in MDA-MB-231 cells as well as to inhibit cell migration, showing good therapeutic potential on TNBC.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Discovery and optimization of withangulatin A derivatives as novel glutaminase 1 inhibitors for the treatment of triple-negative breast cancer

Wu-Xi Zhou et al.

Summary: A potential novel GLS1 inhibitor has been developed through synthesis and optimization, showing effective therapeutic effects on triple-negative breast cancer. The inhibitor induces apoptosis in MDA-MB-231 cells by influencing metabolic pathways. Animal model experiments demonstrate significant therapeutic effects of the inhibitor.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Design, synthesis and evaluation of calix[4]arene-based carbonyl amide derivatives with antitumor activities

Lin An et al.

Summary: Calixarenes have been explored for the design of anticancer agents, leading to the discovery of a series of promising carbonyl amide derivatives with compound 5h showing superior inhibitory effects on lung adenocarcinoma and breast cancer cells while demonstrating low toxicity to normal cells. Mechanism studies indicated that compound 5h could induce cell cycle arrest and apoptosis, suggesting its potential as a novel anticancer drug.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Design, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer

Md Ashraf-Uz-Zaman et al.

Summary: Triple-negative breast cancer is an aggressive type of cancer with high metastatic rates and good responses to chemotherapy, indicating potential for future treatment of metastatic breast cancer using novel compounds.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones

Lan Luo et al.

Summary: The newly synthesized compound 6a has shown promising anticancer activity by inhibiting cell growth and inducing apoptosis in vitro, as well as suppressing tumor growth in vivo, indicating its potential as a future anticancer agent.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Synthesis and in vitro evaluation of novel spiroketopyrazoles as acetyl-CoA carboxylase inhibitors and potential antitumor agents

Tonghui Huang et al.

Summary: A series of spiroketopyrazole derivatives were synthesized and evaluated for their anticancer activities as ACC inhibitors. Compound 7j showed the strongest enzyme inhibitory activity, while compound 7m exhibited potent anti-proliferative effects against various cancer cell lines, indicating its potential as a therapeutic agent for hepatocellular carcinoma.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Multidisciplinary Sciences

Frequency-dependent interactions determine outcome of competition between two breast cancer cell lines

Audrey R. Freischel et al.

Summary: Tumors are dynamic ecosystems where cancer cell subpopulations compete for space and resources. In experiments with MCF-7 and MDA-MB-231 breast cancer cells, MCF-7 cells showed better growth rates and carrying capacities under certain conditions, but were not always able to outcompete MDA-MB-231 cells. The study suggests a reliance on frequency-dependent interactions in understanding competition dynamics among cancer cells.

SCIENTIFIC REPORTS (2021)

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Article Biochemistry & Molecular Biology

2D-and 3D-QSAR modelling, molecular docking and in vitro evaluation studies on 18β-glycyrrhetinic acid derivatives against triple-negative breast cancer cell line

Aparna Shukla et al.

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS (2020)

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Article Chemistry, Medicinal