Discovery of a potent and highly fluorescent sirtuin inhibitor

Y. K. Yoon, M. A. Ali, A. C. Wei, T. S. Choon, A. N. Shirazi, K. Parang

Research output: Contribution to journalArticlepeer-review

Abstract

In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series (BZD9L1) was discovered to show high autofluorescence which can be utilized to predict its localization in cells. More importantly, BZD9L1 displayed strong antiproliferative effects against a panel of cancer cells tested. Molecular docking studies also help to explain the observed structure-activity relationship.

Original languageEnglish (US)
Pages (from-to)1857-1863
Number of pages7
JournalMedChemComm
Volume6
Issue number10
DOIs
StatePublished - 2015
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

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