Discovery of a potent and highly fluorescent sirtuin inhibitor. Issue 10 (15th September 2015)

• Record Type: Journal Article
• Authors: Yoon, Y. K.; Ali, M. A.; Wei, A. C.; Choon, T. S.; Shirazi, A. N.; Parang, K.
• Is Part Of: MedChemComm. Volume 6:Issue 10(2015:Oct.)
• Page Start: 1857
• Page End: 1863
• Publication Date: 2015-09-15
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c5md00307e
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : Highly fluorescent sirtuin inhibitor was discovered to possess growth inhibitory effect against multiple cancer cell lines. 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.