Biologically-validated HIV integrase inhibitors with nucleobase scaffolds: structure, synthesis, chemical biology, molecular modeling, and antiviral activity

V Nair, V Uchil, G Chi, I Dams, A Cox…

Index: Nair, Vasu; Uchil, Vinod; Chi, Guochen; Dams, Iwona; Cox, Arthur; Seo, Byung Nucleosides, Nucleotides and Nucleic Acids, 2007 , vol. 26, # 6-7 p. 665 - 668

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Abstract

Integrase, an enzyme of the pol gene of HIV, is a significant viral target for the discovery of anti-HIV agents. In this presentation, we report on the continuation of our work on the discovery of diketo acids, constructed on nucleobase scaffolds, that are inhibitors of HIV integrase. An example of our synthetic approach to inhibitors with purine nucleobase scaffolds is given. Comparison is made between integrase inhibition data arising from ...