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Title: Structural modification of diketo acid portion in 1h-benzylindole derivatives hiv-1 integrase inhibitors
Authors: Ferro, Stefania ×
De Grazia, Sara
De Luca, Laura
Barreca, Maria Letizia
Debyser, Zeger
Chimirri, Alba #
Issue Date: Apr-2009
Publisher: Pergamon-elsevier science ltd
Series Title: Heterocycles vol:78 issue:4 pages:947-959
Abstract: Our previous studies led to discovery of a very potent benzylindoldiketo acid (CHI-1043) acting as HIV-1 integrase strand transfer inhibitor. We herein report the synthesis of new structurally different compounds in which the 1,3-diketo acid moiety has been substituted with other functionalities. The synthesized derivatives were evaluated for their activity on the IN enzyme and in MT-4 cells but only 4-[1-(4-fluorobenzyl)-4-methoxy-1H-indol-3-yl)-3-hydroxyfuran-2(5H)-one (12) was able to strongly inhibit HIV-1 probably by biotransformation into CHI-1043.
ISSN: 0385-5414
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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