Contrasting sirtuin and poly(ADP-ribose)polymerase activities of selected 2,4,6-trisubstituted benzimidazoles

Yeong, Keng Yoon and Tan, Soo Choon and Mai, Chun-Wai and Leong, Chee-Onn and Chung, Felicia Fei-Lei and Lee, Yean Kee and Chee, Chin Fei and Abd Rahman, Noorsaadah (2017) Contrasting sirtuin and poly(ADP-ribose)polymerase activities of selected 2,4,6-trisubstituted benzimidazoles. Chemical Biology and Drug Design, 91 (1). pp. 213-219. ISSN 1747-0277

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Both sirtuin and poly(ADP-ribose)polymerase (PARP) family of enzymes utilize NAD+ as co-substrate. Inhibitors of sirtuins and PARPs are important tools in drug discovery as they are reported to be linked to multiple diseases such as cancer. New potent sirtuin inhibitors (2,4,6-trisubstituted benzimidazole) were discovered from reported PARP inhibitor scaffold. Interestingly, the synthesized compounds have contrasting sirtuin and PARP-1 inhibitory activities. We showed that modification on benzimidazoles may alter their selectivity toward sirtuin or PARP-1 enzymes. This offers an opportunity for further discovery and development of new promising sirtuin inhibitors. Molecular docking studies were carried out to aid the rationalization of these observations. Preliminary antiproliferative studies of selected compounds against nasopharyngeal cancer cells also showed relatively promising results.

Item Type: Article
Uncontrolled Keywords: anticancer; benzimidazole; molecular docking; nasopharyngeal; poly(ADP-ribose) polymerases; sirtuin
Subjects: Q Science > Q Science (General)
Q Science > QD Chemistry
R Medicine
Divisions: Faculty of Science > Dept of Chemistry
Depositing User: Ms. Juhaida Abd Rahim
Date Deposited: 12 Feb 2019 08:44
Last Modified: 12 Feb 2019 08:44

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