Bifunctional inhibition of HIV-1 reverse transcriptase: a first step in designing a bifunctional triphosphate

D Piao, A Basavapathruni, P Iyidogan, G Dai…

Index: Piao, Dongyuan; Basavapathruni, Aravind; Iyidogan, Pinar; Dai, Guangxiu; Hinz, Wolfgang; Ray, Adrian S.; Murakami, Eisuke; Feng, Joy Y.; You, Fei; Dutschman, Ginger E.; Austin, David J.; Parker, Kathlyn A.; Anderson, Karen S. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 5 p. 1511 - 1518

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Citation Number: 3

Abstract

The onset of resistance to approved anti-AIDS drugs by HIV necessitates the search for novel inhibitors of HIV-1 reverse transcriptase (RT). Developing single molecular agents concurrently occupying the nucleoside and nonnucleoside binding sites in RT is an intriguing idea but the proof of concept has so far been elusive. As a first step, we describe molecular modeling to guide focused chemical syntheses of conjugates having ...