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 & Drug Design, 91 (1). pp. 213-219. ISSN 1747-0277, DOI https://doi.org/10.1111/cbdd.13072.
Full text not available from this repository.Abstract
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 |
|---|---|
| Funders: | Monash University Malaysia SEED Fund, RUC Research Grant (1001/PSK/8620012) |
| 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 > Department of Chemistry |
| Depositing User: | Ms. Juhaida Abd Rahim |
| Date Deposited: | 12 Feb 2019 08:44 |
| Last Modified: | 26 Aug 2019 02:22 |
| URI: | http://eprints.um.edu.my/id/eprint/20276 |
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