Title: Nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity
Authors: Yu, Shenghui
Zhang, Linna
Yan, Shifeng
Wang, Peng
Sanchez, Tino
Christ, Frauke
Debyser, Zeger
Neamati, Nouri ×
Zhao, Guisen #
Issue Date: Jan-2012
Publisher: Taylor & Francis
Series Title: Journal of Enzyme Inhibition and Medicinal Chemistry vol:27 issue:5 pages:628-640
Abstract: Four series of forty-five nitrogen-containing polyhydroxylated aromatics based on caffeic acid phenethyl ester were designed and synthesized as HIV-1 integrase (IN) inhibitors. Most of these compounds inhibited IN catalytic activities in low micromolar range. Among these new analogues, compounds 9e and 9f were the most potent IN inhibitors with IC(50) value of 0.7 μM against strand transfer reaction. Their key structure-activity relationships were also discussed.
ISSN: 1475-6366
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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