☆ 4.5 Article

Synthesis and anti-HIV activity novel nucleoside phosphonate HIV of GS-9148 (2′-Fd4AP), a reverse transcriptase inhibitor

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Volume 18, Issue 3, Pages 1120-1123

Publisher

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2007.11.125

Keywords

HIV; phosphonate; antiviral; resistance

Categories

Chemistry, Medicinal Chemistry, Organic

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Abstract

GS-9148 (2'-Fd4AP, 4) has been identified as a nucleoside phosphonate reverse transcriptase (RT) inhibitor with activity against wild-type HIV (EC50 = 12 mu M). Unlike many clinical RT inhibitors, relevant reverse transcriptase mutants (M184V, K65R, 6-TAMs) maintain a susceptibility to 2'-Fd4AP that is similar to wild-type virus. The 2'-fluorine group was rationally designed into the molecule to improve the selectivity profile and in preliminary studies using HepG2 cells, compound 4 showed no measurable effect on mitochondrial DNA content indicating a low potential for mitochondrial toxicity. (C) 2007 Elsevier Ltd. All rights reserved.

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