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Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.

Chen, P; Cheng, P T; Alam, M; Beyer, B D; Bisacchi, G S; Dejneka, T; Evans, A J; Greytok, J A; Hermsmeier, M A; Humphreys, W G; Jacobs, G A; Kocy, O; Lin, P F; Lis, K A; Marella, M A; Ryono, D E; Sheaffer, A K; Spergel, S H; Sun, C Q; Tino, J A; Vite, G; Colonno, R J; Zahler, R; Barrish, J C.

J Med Chem ; 39(10): 1991-2007, 1996 May 10.

Artículo en Inglés | MEDLINE | ID: mdl-8642558

RESUMEN

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 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 and in cell culture) compounds (10l, 10m, 10n, and 15c) which possess significantly decreased cytotoxicity.

Asunto(s)

Aminas/síntesis química , Inhibidores de la Proteasa del VIH/síntesis química , Aminas/química , Aminas/farmacología , División Celular/efectos de los fármacos , Línea Celular , Supervivencia Celular/efectos de los fármacos , Inhibidores de la Proteasa del VIH/química , Inhibidores de la Proteasa del VIH/farmacología , Humanos , Relación Estructura-Actividad

RESUMEN

Asunto(s)

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