Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596416 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives were investigated as novel small molecule amplifiers of heat shock factor 1 transcriptional activity. Lead optimization led to the discovery of compound 4A-13, which displayed potent HSF1 activity under mild heat stress (EC50 = 2.5 μM) and significant cytoprotection in both rotenone (EC50 = 0.23 μM) and oxygen-glucose deprivation cell toxicity models (80% protection at 2.5 μM).
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yuefen Zhou, Linyi Wei, Thomas P. Brady, P.S. Murali Mohan Redddy, Tram Nguyen, Jinhua Chen, Qingyan Au, Il Sang Yoon, Gary Yip, Bin Zhang, Jack R. Barber, Shi Chung Ng,