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Issue 12, 2019
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Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives

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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.

Graphical abstract: Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives

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Supplementary files

Article information


Submitted
08 Jun 2019
Accepted
28 Oct 2019
First published
18 Nov 2019

Med. Chem. Commun., 2019,10, 2140-2145
Article type
Research Article

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

K. Y. Yeong, M. I. H. Nor Azizi, N. Berdigaliyev, W. N. Chen, W. L. Lee, A. N. Shirazi and K. Parang, Med. Chem. Commun., 2019, 10, 2140
DOI: 10.1039/C9MD00323A

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