Design, Synthesis and Biological Evaluation of Novel 5- Phenyl-5-(thiophen-2-yl)-4H-1,2,4-triazole-3-thiols as an Anticancer Agent

摘要

Tumor suppressor protein p53 is one of the most appealing targets for targeted anticancer therapy, due to its significant role in cancer prevention and abundant mutation in human cancers. A novel series of 4-phenyl-5-(thiophen-2-yl)-4H-1,2,4- triazole-3-thiols having ability to liberate p53 function by interrupting p53-MDM2 interaction were successfully discov- ered by structure-based designing approach and the principle of bioisosterism. In silico modules predicted that these small molecule inhibitors comprising 1,2,4-triazole-3-thiol scaffold have draggability and ability to mimic critical binding residues of p53.