Discovery of a potent and highly fluorescent sirtuin inhibitor. Issue 10 (15th September 2015) - Yoon, Y. K.
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.