Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives as novel small molecule chaperone amplifiers.
Basic Information
ID: ALA1152353
Journal: Bioorg Med Chem Lett
Title: Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives as novel small molecule chaperone amplifiers.
Authors: Zhou Y, Wei L, Brady TP, Murali Mohan Redddy PS, Nguyen T, Chen J, Au Q, Yoon IS, Yip G, Zhang B, Barber JR, Ng SC.
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 (EC(50)=2.5microM) and significant cytoprotection in both rotenone (EC(50)=0.23microM) and oxygen-glucose deprivation cell toxicity models (80% protection at 2.5microM).
CiteXplore: 19502057
DOI: 10.1016/j.bmcl.2009.05.073
Patent ID: ┄