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

Yeong KY 1 , Nor Azizi MIH 1 , Berdigaliyev N 1 , Chen WN 1 , Lee WL 1 , Shirazi AN 2 Show all authors , Parang K 2

Affiliations 

  • 1 School of Science , Monash University Malaysia , Jalan Lagoon Selatan , Bandar Sunway , 47500 , Selangor , Malaysia . Email: yeong.kengyoon@monash.edu
  • 2 Department of Biomedical and Pharmaceutical Sciences , College of Pharmacy , University of Rhode Island , Kingston , RI 02881 , USA
Medchemcomm, 2019 Dec 01;10(12):2140-2145.
PMID: 32904142 DOI: 10.1039/c9md00323a

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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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