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Molecules 2010, 15(5), 3048-3078;

Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors

LBPA, CNRS, Ecole Normale Supérieure de Cachan, France
Faculté de Pharmacie, Université Paris-Sud, UMR CNRS 8076 BIOCIS, Châtenay-Malabry, France
Author to whom correspondence should be addressed.
Received: 2 March 2010 / Revised: 8 April 2010 / Accepted: 12 April 2010 / Published: 27 April 2010
(This article belongs to the Special Issue Anti-Infective Agents)
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In spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still suffers from deleterious side effects and emerging drug resistance. Therefore, the development of novel antiviral drugs remains a crucial issue for the fight against AIDS. HIV-1 integrase is a key enzyme in the replication cycle of the retrovirus since it catalyzes the integration of the reverse transcribed viral DNA into the chromosomal DNA. Efforts to develop anti-integrase drugs started during the early nineties, culminating with the recent approval of Raltegravir. The discovery and the development of the styrylquinoline inhibitor class was an important step in the overall process. In this review we have described the key synthetic issues and the structure-activity relationship of this family of integrase inhibitors. Crystallographic and docking studies that shed light on their mechanism of action are also examined. View Full-Text
Keywords: AIDS; HIV-1; integrase; inhibitor; styrylquinoline AIDS; HIV-1; integrase; inhibitor; styrylquinoline

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Mouscadet, J.-F.; Desmaële, D. Chemistry and Structure-Activity Relationship of the Styrylquinoline-Type HIV Integrase Inhibitors. Molecules 2010, 15, 3048-3078.

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