Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591070 | Bioorganic & Medicinal Chemistry Letters | 2014 | 18 Pages |
Abstract
A novel class of phenyl benzenesulfonylhydrazides has been identified as potent inhibitors of indoleamine 2,3-dioxygenase (IDO), and their structure-activity relationship was explored. Coupling reactions between various benzenesulfonyl chlorides and phenylhydrazides were utilized to synthesize the sulfonylhydrazides bearing various substituents. Compound 3i exhibited 61Â nM of IC50 in enzymatic assay and 172Â nM of EC50 in the HeLa cell. The computational study of 3i suggested that the major interactions between 3i and IDO protein are the coordination of sulfone and heme iron, the hydrogen bonding and hydrophobic interactions between 3i and IDO. This novel class of IDO inhibitor provides a new direction to discover effective anti-cancer agents.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ming-Fu Cheng, Ming-Shiu Hung, Jen-Shin Song, Shu-Yu Lin, Fang-Yu Liao, Mine-Hsine Wu, Wenchi Hsiao, Chia-Ling Hsieh, Jian-Sung Wu, Yu-Sheng Chao, Chuan Shih, Su-Ying Wu, Shau-Hua Ueng,