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Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives.

ABSTRACT: New benzimidazoles were synthesized based on the previously identified sirtuin inhibitor BZD9L1. The compounds were screened for their sirtuin (SIRT1, SIRT2 and SIRT3) inhibitory activities. Compound BZD9Q1 was determined to be a pan-SIRT1-3 inhibitor. Furthermore, the proliferation of various cancer cells was inhibited by BZD9Q1. It was shown that BZD9Q1 elicits a cytostatic effect by inducing cell cycle arrest at the G2/M phase while also showing a prominent induction of apoptosis against oral cancer cells.

SUBMITTER: Yeong KY

PROVIDER: S-EPMC7451065 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives.

Yeong K Y KY Nor Azizi M I H MIH Berdigaliyev N N Chen W N WN Lee W L WL Shirazi A N AN Parang K K

MedChemComm 20191118 12

New benzimidazoles were synthesized based on the previously identified sirtuin inhibitor BZD9L1. The compounds were screened for their sirtuin (SIRT1, SIRT2 and SIRT3) inhibitory activities. Compound BZD9Q1 was determined to be a pan-SIRT1-3 inhibitor. Furthermore, the proliferation of various cancer cells was inhibited by BZD9Q1. It was shown that BZD9Q1 elicits a cytostatic effect by inducing cell cycle arrest at the G2/M phase while also showing a prominent ind ...[more]

PMID: 32904142

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