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; K. Parang

doi:10.1039/C9MD00323A

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

K. Y. Yeong,

*^a M. I. H. Nor Azizi,^a N. Berdigaliyev,

^a W. N. Chen,^a W. L. Lee,*^a A. N. Shirazi^bcd and K. Parang^bd

Author affiliations

* Corresponding authors

^a School of Science, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor, Malaysia
E-mail: yeong.kengyoon@monash.edu

^b Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI, USA

^c Department of Pharmaceutical Sciences, College of Pharmacy, Marshall B. Ketchum University, Fullerton, CA 92831, USA

^d Center for Targeted Drug Delivery, Department of Biomedical and Pharmaceutical Sciences, Chapman University School of Pharmacy, Harry and Diane Rinker Health Science Campus, Irvine, CA 92618, USA

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.

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Article information

DOI: https://doi.org/10.1039/C9MD00323A
Article type: Research Article
Submitted: 08 Jun 2019
Accepted: 28 Oct 2019
First published: 18 Nov 2019

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Med. Chem. Commun., 2019,10, 2140-2145

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

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

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