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American Chemical Society, Journal of Medicinal Chemistry, 15(51), p. 4744-4750, 2008

DOI: 10.1021/jm8001422

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Novel Quinolinonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, and Biological Activities

Journal article published in 2008 by Roberto Di Santo ORCID, Roberta Costi ORCID, Alessandra Roux, Gaetano Miele, Giuliana Cuzzucoli Crucitti, Alberto Iacovo, Federica Rosi, Antonio Lavecchia, Luciana Marinelli, Carmen Di Giovanni, Ettore Novellino, Lucia Palmisano, M. Andreaotti, Mauro Andreotti, Roberta Amici and other authors.
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

Novel quinolinonyl diketo acids were designed to obtain integrase (IN) inhibitors selectively active against the strand transfer (ST) step of the HIV integration process. Those new compounds are characterized by a single aryl diketo acid (DKA) chain in comparison to 4, a bifunctional diketo acid reported by our group as an anti-IN agent highly potent against both the 3'-processing and ST steps. Compound 6d was the most potent derivative in IN enzyme assays, while 6i showed the highest potency against HIV-1 in acutely infected cells. The selective inhibition of ST suggested the newly designed monofunctional DKAs bind the IN-DNA acceptor site without affecting the DNA donor site.