Discovery of a potent and highly fluorescent sirtuin inhibitor†
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.
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