Benzimidazole based bis-carboxamide derivatives as promising cytotoxic agents: Design, synthesis, in silico and tubulin polymerization inhibition

Kritika Laxmikeshav,Pooja Sharma, Manisurya Palepu,Pravesh Sharma,Ashutosh Mahale,Joel George,Regur Phanindranath,Manoj P. Dandekar,Onkar Prakash Kulkarni,Narayana Nagesh,Nagula Shankaraiah

Journal of Molecular Structure（2023）

引用 12|浏览10

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摘要

•Carboxamide-based benzimidazoles were synthesized via “acid-amine coupling”•Compounds 10g and 10m showed significant cytotoxicity on SK-Mel-28 cell line•10g and 10m induced tubulin polymerization inhibition, DNA intercalation and G2/M cell cycle arrest•Collapse of DΨm and increased the levels of superoxide ROS was observed

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关键词

Anti-cancer,Benzimidazole,Carboxamide,DNA intercalation,Tubulin inhibition,Structure-activity relationship (SAR)

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