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Title: Synthesis and anti-HIV activity of a bile acid analog of cosalane
Authors: Kannan, A ×
De Clercq, Erik
Pannecouque, Christophe
Witvrouw, Myriam
Hartman, T
Turpin, J
Buckheit, R
Cushman, M #
Issue Date: 2001
Series Title: Tetrahedron vol:57 pages:9385-9391
Abstract: Cosalane is a novel anti-HIV agent that inhibits the attachment of gp120 to CD4. The therapeutic potential of cosalane is limited by poor oral absorption. In an attempt to target the ileal bile acid transporter and thus facilitate oral bioavailability, a cosalane analog was synthesized in which the disalicylmethane pharmacophore is attached to a bile acid through a linker chain appended to C-17 of the steroid nucleus. The resulting bile acid analog of cosalane, retained antiviral activity vs. HIV-1(IIIB) and HIV-2(ROD) in MT-4 cells, but was less potent than cosalane. (C) 2001 Elsevier Science Ltd. All rights reserved.
ISSN: 0040-4020
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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