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Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors.

ABSTRACT: A set of novel diarylpyridines as anti-tubulin agents were designed, synthesised using a rigid pyridine as a linker to fix the cis-orientation of ring-A and ring-B. All of the target compounds were evaluated for their in vitro antiproliferative activities. Among them, 10t showed remarkable antiproliferative activities against three cancer cell lines (HeLa, MCF-7 and SGC-7901) in sub-micromolar concentrations. Consistent with its potent antiproliferative activity, 10t also displayed potent anti-tubulin activity. Cellular mechanism investigation elucidated 10t disrupted the cellular microtubule structure, arrested cell cycle at G2/M phase and induces apoptosis. Molecular modelling studies showed that 10t could bind to the colchicine binding site on microtubules. These results provide motivation and further guidance for the development of new CA-4 analogues.

SUBMITTER: Yang S

PROVIDER: S-EPMC9553186 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature

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Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors.

Yang Shanbo S Wang Chao C Shi Lingyu L Chang Jing J Zhang Yujing Y Meng Jingsen J Liu Wenjing W Zeng Jun J Zhang Renshuai R Shao Yingchun Y Xing Dongming D

Journal of enzyme inhibition and medicinal chemistry 20221201 1

A set of novel diarylpyridines as anti-tubulin agents were designed, synthesised using a rigid pyridine as a linker to fix the cis-orientation of ring-A and ring-B. All of the target compounds were evaluated for their in vitro antiproliferative activities. Among them, 10t showed remarkable antiproliferative activities against three cancer cell lines (HeLa, MCF-7 and SGC-7901) in sub-micromolar concentrations. Consistent with its potent antiproliferative activity, 10t ...[more]

PMID: 36196773

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Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors.

Publications

Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors.

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