Document 0611
 DOCN  M9550611
 TI    Cosalane analogues with enhanced potencies as inhibitors of HIV-1
       protease and integrase.
 DT    9505
 AU    Cushman M; Golebiewski WM; Pommier Y; Mazumder A; Reymen D; De Clercq E;
       Graham L; Rice WG; Department of Medicinal Chemistry and Pharmacognosy,
       School of; Pharmacy and Pharmacal Sciences, Purdue University, West;
       Lafayette, Indiana 47907.
 SO    J Med Chem. 1995 Feb 3;38(3):443-52. Unique Identifier : AIDSLINE
       MED/95156420
 AB    Several new analogues of the novel anti-HIV agent cosalane have been
       synthesized and evaluated as inhibitors of HIV-1 integrase and protease,
       HIV-1 replication, HIV-1 and HIV-2 cytopathicity, HIV-1- and
       HIV-2-mediated syncytium formation, and cytopathicity of a variety of
       human pathogenic viruses. The congeners displayed enhanced potencies
       relative to cosalane itself as inhibitors of HIV-1 integrase and
       protease. The two most potent analogues against HIV-1 integrase
       displayed IC50 values of 2.2 microM, while the three most potent
       compounds against HIV-1 protease had IC50 values in the 0.35-0.39 microM
       range. In addition to its activity against HIV-1 and HIV-2
       cytopathicity, cosalane inhibited the cytopathic effects of herpes
       simplex virus-1, herpes simplex virus-2, and human cytomegalovirus at
       concentrations that were well below the cytotoxic concentrations.
       Potentially useful antiviral activities were also revealed for some of
       the new cosalane congeners against influenza virus, Junin virus, and
       Tacaribe virus.
 DE    Amino Acid Sequence  Antiviral Agents/*PHARMACOLOGY  Aurintricarboxylic
       Acid/*ANALOGS & DERIVATIVES/CHEMISTRY/  PHARMACOLOGY  Cell Line  DNA
       Nucleotidyltransferases/*ANTAGONISTS & INHIB  Herpesviridae/DRUG EFFECTS
       Human  HIV Protease Inhibitors/*PHARMACOLOGY  HIV-1/*DRUG
       EFFECTS/ENZYMOLOGY/PHYSIOLOGY  Microbial Sensitivity Tests  Molecular
       Sequence Data  Support, Non-U.S. Gov't  Support, U.S. Gov't, P.H.S.
       Virus Replication/DRUG EFFECTS  JOURNAL ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
       protected by Copyright Law (Title 17, U.S.Code).