Synthesis and evaluation of novel benzimidazole derivatives as sirtuin inhibitors with antitumor activities

Yeong Keng Yoon, Mohamed Ashraf Ali, Ang Chee Wei, Tan Soo Choon, Hasnah Osman, Keykavous Parang, Amir Nasrolahi Shirazi

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41 Citations (Scopus)


A total of 15 novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. All compounds showed better inhibition on SIRT2 as compared to SIRT1. Among these, compound 5j displayed the best inhibitory activity for SIRT1 (IC50 = 58.43 μM) as well as for SIRT2 (IC50 = 45.12 μM). Cell cytotoxicity assays also showed that compound 5j possesses good antitumor activity against two different cancer cell lines derived from breast cancer (MCF-7 and MDA-MB-468). A simple structure-activity-relationship (SAR) study of the newly synthesized benzimidazole derivatives was also discussed.

Original languageEnglish
Pages (from-to)703-710
Number of pages8
JournalBioorganic & Medicinal Chemistry
Issue number2
Publication statusPublished - 15 Jan 2014
Externally publishedYes


  • Anti-proliferative
  • Benzimidazole
  • Breast cancer
  • Electron donating
  • Sirtuin

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