32245-26-4Relevant academic research and scientific papers
Synthesis, anticancer activity and molecular docking studies on 1,2-diarylbenzimidazole analogues as anti-tubulin agents
Zhang, Ya-Liang,Yang, Rong,Xia, Lin-Ying,Man, Ruo-Jun,Chu, Yi-Chun,Jiang, Ai-Qin,Wang, Zhong-Chang,Zhu, Hai-Liang
, (2019)
Twenty-four 1,2-diarylbenzimidazole derivatives were designed, synthesized and biologically evaluated. It turned out that most of them were potential anticancer drugs. Among them, compound c24 showed the highest anti-tumor activity (GI50 = 0.71–2.41 μM against HeLa, HepG2, A549 and MCF-7 cells), and low toxicity to normal cells (CC50 > 100 μM against L02 cells). In the microtubule binding assay, c24 showed the most potent inhibition of microtubule polymerization (IC50 = 8.47 μM). The binding ability of compound c24 to tubulin crystal was verified by molecular docking simulation experiment. Further studies on HepG2 and HeLa cells showed that compound c24 could cause mitotic arrest of tumor cells to G2/M phase then inducing apoptosis. To sum up, compound c24 is a promising microtubule assembly inhibitor.
Preparation of 1,2-diaryl benzimidazole derivative and application thereof
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Paragraph 0018-0021, (2019/01/13)
The invention discloses a preparation method of a novel microtubular inhibitor 1,2-diaryl benzimidazole derivative and application thereof to the anti-tumor aspect. The 1,2-diaryl benzimidazole derivative has the structure shown in the formula I: the form
