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

Keng Yoon Yeong, Soo Choon Tan, Chun Wai Mai, Chee Onn Leong, Felicia Fei Lei Chung, Yean Kee Lee, Chin Fei Chee, Noorsaadah Abdul Rahman

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)213-219
Number of pages7
JournalChemical Biology & Drug Design
Issue number1
Publication statusPublished - Jan 2018


  • anticancer
  • benzimidazole
  • molecular docking
  • nasopharyngeal
  • poly(ADP-ribose) polymerases
  • sirtuin

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