Aminodiol HIV Protease Inhibitors. Synthesis And Structure-Activity Relationships Of P1/P1'Compounds: Correlation between Lipophilicity and Cytotoxicity

…, AJ Evans, JA Greytok, MA Hermsmeier…

Index: Chen, Ping; Cheng, Peter T. W.; Alam, Masud; Beyer, Barbara D.; Bisacchi, Gregory S.; Dejneka, Tamara; Evans, Adelaide J.; Greytok, Jill A.; Hermsmeier, Mark A.; Humphreys, W. Griffith; Jacobs, Glenn A.; Kocy, Octavian; Lin, Pin-Fang; Lis, Karen A.; Marella, Michael A.; Ryono, Denis E.; Sheaffer, Amy K.; Spergel, Steven H.; Sun, Chong-Qing; Tino, Joseph A.; Vite, Gregory; Colonno, Richard J.; Zahler, Robert; Barrish, Joel C. Journal of Medicinal Chemistry, 1996 , vol. 39, # 10 p. 1991 - 2007

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Citation Number: 48

Abstract

A series of novel aminodiol inhibitors of HIV protease based on the lead compound 1 with structural modifications at P1'were synthesized in order to reduce the cytotoxicity of 1. We have observed a high degree of correlation between the lipophilicity and the cytotoxicity of this series of inhibitors. It was found that appropriate substitution at the para position of the P1'phenyl group of 1 resulted in the identification of equipotent (both against the enzyme ...