Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents
Qifan Zhou, Lina Jia, Fangyu Du, Xiaoyu Dong, Wanyu Sun, Lihui Wang, Guoliang Chen
Abstract
A novel series of pyrrole-3-carboxamides targeting EZH2 have been designed and synthesized. The structure–activity relationships were summarized by combining with<italic>in vitro</italic>biological activity assay and docking results.
Topics & Concepts
ChemistryCarboxamidePyrroleEZH2In vitroEnhancerBiological activityDocking (animal)Combinatorial chemistryStereochemistryBiochemistryMethylationOrganic chemistryTranscription factorNursingMedicineGeneEpigenetics and DNA MethylationChemical Reactions and IsotopesDNA and Nucleic Acid Chemistry