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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: Pyrimido [5,4-e][1,2,4] triazine-5,7 (1H,6H)-dione derivatives as novel small molecule chaperone amplifiers. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4303-7. Epub 2009 May 27.
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). |
7(0,0,1,2) |