Sirtuin Inhibition and Anti-Cancer Activities of Ethyl 2-benzimidazole-5-carboxylate Derivatives

Authors

K. Y. Yeong, Monash University Malaysia
M. I. H. Nor Azizi, Monash University Malaysia
N. Berdigaliyev, Monash University Malaysia
W. N. Chen, Monash University Malaysia
W. L. Lee, Monash University Malaysia
Amir Nasrolahi Shirazi, Chapman UniversityFollow
Keykavous Parang, Chapman UniversityFollow

Document Type

Article

Publication Date

11-18-2019

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.

Comments

This article was originally published in Medchemcomm, volume 10, issue 12, in 2019. https://doi.org/10.1039/c9md00323a

Recommended Citation

Yeong KY, Nor Azizi MIH, Berdigaliyev N, et al. Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives. Medchemcomm. 2019;10(12):2140-2145. https://doi.org/10.1039/c9md00323a

Copyright

Royal Society of Chemistry