252004-32-3Relevant academic research and scientific papers
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency
Bollini, Mariela,Gallardo-Macias, Ricardo,Spasov, Krasimir A.,Tirado-Rives, Julian,Anderson, Karen S.,Jorgensen, William L.
, p. 1110 - 1113 (2013/03/14)
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved activity towards Tyr181Cys containing variants was pursued with the assistance of free energy perturbation (FEP) calculations. Optimization of the 4-R substituent in 1 led to ethyl and isopropyl analogs 1e and 1f with 1-7 nM potency towards both the wild-type virus and a Tyr181C variant.
Isothiazole derivatives useful as anticancer agents
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, (2008/06/13)
The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2and R3are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
