srt1720 and Breast-Neoplasms

Human sirtuin 2 (SIRT2) plays pivotal roles in multiple biological processes such as cell cycle regulation, autophagy, immune and inflammatory responses. Dysregulation of SIRT2 was considered as a main aspect contributing to several human diseases, including cancer. Development of new potent and selective SIRT2 inhibitors is currently desirable, which may provide a new strategy for treatment of related diseases. Herein, a structure-based optimization approach led to new 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as SIRT2 inhibitors. SAR analyses with new synthesized derivatives revealed a number of new potent SIRT2 inhibitors, among which 28e is the most potent inhibitor with an IC

Topics: Acetamides; Antineoplastic Agents; Breast; Breast Neoplasms; Drug Discovery; Female; Histone Deacetylase Inhibitors; Humans; MCF-7 Cells; Molecular Docking Simulation; Pyrimidines; Sirtuin 2; Structure-Activity Relationship; Tubulin