Synthesis and evaluation of 2‐aryl‐1H‐benzoimidazole derivatives as potential microtubule targeting agents

Microtubule targeting agents (MTAs) are the potential drug candidates for anticancer drug discovery. Disrupting the microtubule formation or inhibiting the de‐polymerization process by a synthetic molecule can lead to an excellent anticancer drug candidate. Here, we present the 2,5‐substituted‐1H‐be...

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Bibliographic Details
Published in:Drug development research 2022-05, Vol.83 (3), p.769-782
Main Authors: Jung‐Seop Lee, In‐ho Song, Warkad, Shrikant Dashrath, Yeom, Gyu Seong, Shinde, Pramod B, Keum‐soo Song, Nimse, Satish Balasaheb
Format: Article
Language:English
Subjects:
Anticancer properties
Antitumor activity
Antitumor agents
Benzimidazoles
Binding sites
Cancer
Cell lines
Chemical synthesis
Colchicine
Drug development
Imidazole
Lead compounds
Metabolism
Nocodazole
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Summary:Microtubule targeting agents (MTAs) are the potential drug candidates for anticancer drug discovery. Disrupting the microtubule formation or inhibiting the de‐polymerization process by a synthetic molecule can lead to an excellent anticancer drug candidate. Here, we present the 2,5‐substituted‐1H‐benzo[d]imidazole derivatives as potential colchicine, nocodazole binding site targeting agents. About 20 benzimidazole derivatives were synthesized with 82.0%–94.0% yield using mild reaction conditions. The synthesized compounds showed moderate to excellent anticancer activity established in three cell lines, including Hela cells, A549 cells, MRC‐5 cells. The compounds B15, B16, B19, and B20 are the potential candidates with the IC50 values
ISSN:0272-4391
1098-2299
DOI:10.1002/ddr.21909