Sirtuin Inhibition and Anti-Cancer Activities of Ethyl 2-benzimidazole-5-carboxylate Derivatives
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.
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
Royal Society of Chemistry