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American Chemical Society, Journal of Medicinal Chemistry, 4(58), p. 1915-1928, 2015

DOI: 10.1021/jm501799k

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Structure–Activity Relationship of Pyrrolyl Diketo Acid Derivatives as Dual Inhibitors of HIV-1 Integrase and Reverse Transcriptase Ribonuclease H Domain

Journal article published in 2015 by Giuliana Cuzzucoli Crucitti, Mathieu Métifiot, Luca Pescatori, Antonella Messore, Valentina Noemi Madia ORCID, Giovanni Pupo, Francesco Saccoliti, Luigi Scipione ORCID, Silvano Tortorella, Francesca Esposito, Angela Corona ORCID, Marta Cadeddu ORCID, Christophe Marchand, Yves Pommier, Enzo Tramontano ORCID and other authors.
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This paper is available in a repository.

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Abstract

The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse transcriptase-associated ribonuclease H (RNase H) are both selective targets for HIV-1 chemotherapy, and the identification of dual IN/RNase H inhibitors is an attractive strategy for new drug development. We newly synthesized pyrrolyl derivatives that exhibited good potency against IN and a moderate inhibition of the RNase H function of RT, confirming the possibility of developing dual HIV-1 IN/RNase H inhibitors and obtaining new information for the further development of more effective dual HIV-1 inhibitors