PMID: 7932526Sep 16, 1994Paper

Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction

Journal of Medicinal Chemistry
M CushmanW G Rice

Abstract

Cosalane (3), a novel anti-HIV agent having a disalicylmethane unit linked to C-3 of cholestane by a three-carbon linker, was synthesized from commercially available starting materials by a convergent route. Cosalane proved to be a potent inhibitor of HIV with a broad range of activity against a variety of laboratory, drug-resistant, and clinical HIV-1 isolates, HIV-2, and Rauscher murine leukemia virus. The cytotoxicity of cosalane is relatively low as reflected by an in vitro therapeutic index of > 100. Although cosalane inhibits HIV-1 reverse transcriptase and protease, time of addition experiments indicate that it prevents the cytopathic effect of HIV by acting earlier than reverse transcription in the viral replication cycle. The available evidence indicates that the primary mechanism of action of cosalane involves inhibition of gp120-CD4 binding as well as inhibition of a postattachment event prior to reverse transcription.

Citations

Jan 5, 2002·International Journal of Pharmaceutics·K R KuchimanchiA K Mitra
Sep 22, 2000·Bioorganic & Medicinal Chemistry Letters·G C PaulM Cushman
Nov 22, 2000·Bioorganic & Medicinal Chemistry Letters·K C SanthoshM Cushman
Jan 5, 2001·Bioorganic & Medicinal Chemistry Letters·O M HowardM Cushman
Jun 12, 2002·Bioorganic & Medicinal Chemistry·Guozhang XuMark Cushman
Sep 1, 2000·Bioorganic & Medicinal Chemistry·A Casimiro-GarciaM Cushman
May 29, 2000·Journal of Pharmaceutical Sciences·D PalA K Mitra
May 1, 2010·Viruses·Jason A Wojcechowskyj, Robert W Doms
Jul 23, 2003·Rapid Communications in Mass Spectrometry : RCM·Maximilian A SilvestriMark Cushman
Aug 8, 2006·ChemMedChem·D Christopher Meadows, Jacquelyn Gervay-Hague
Sep 21, 2018·Frontiers in Immunology·Jon Ander Nieto-GaraiHans-Georg Kräusslich
Feb 7, 2001·Bioorganic Chemistry·K MaurerA D Leavitt
Apr 1, 1995·Clinical Microbiology Reviews·E De Clercq

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