Title: Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors
Authors: Al-Mawsawi, Laith Q
Dayam, Raveendra
Taheri, Laleh
Witvrouw, Myriam
Debyser, Zeger
Neamati, Nouri # ×
Issue Date: Dec-2007
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:17 issue:23 pages:6472-6475
Abstract: The previously discovered salicylhydrazide class of compounds displayed potent HIV-1 integrase (IN) inhibitory activity. The development of this class of compounds as antiretroviral agents was halted due to cytotoxicity in the nanomolar to sub-micromolar range. We identified a novel class of non-cytotoxic hydrazide IN inhibitors utilizing the minimally required salicylhydrazide substructure as a template in a small-molecule database search. The novel hydrazides displayed low micromolar IN inhibitory activity and are several hundred-fold less cytotoxic than previously disclosed salicylhydrazide IN inhibitors.
ISSN: 0960-894X
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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