Publications by authors named "Amit S Shete"
Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR.
Bioorg Med Chem Lett
January 2017
Article Synopsis
- EZH2 is a crucial component of the PRC2 complex, responsible for adding methyl groups to histone H3, which can influence gene expression and is linked to various cancers when dysregulated.
- Developing EZH2 inhibitors has become a key focus in cancer therapy, with many existing inhibitors featuring a bicyclic heteroaryl structure.
- This study presents the creation of new EZH2 inhibitors based on an indoline core, which show strong effectiveness (nanomolar activity) while enhancing solubility and stability against oxidative breakdown.