Article
Modular assembly of purine-like bisphosphonates as inhibitors of HIV-1 reverse transcriptase.
Journal of medicinal chemistry - 11 Sept 2014
Lacbay Cyrus M, Mancuso John, Lin Yih-Shyan, Bennett Nicholas, Götte Matthias, Tsantrizos Youla S
Abstract excerpt
Bisphosphonates can mimic the pyrophosphate leaving group of the nucleotidyl transfer reaction and effectively inhibit RNA/DNA polymerases. In a search of HIV-1 reverse transcriptase (RT) inhibitors, a new chemotype of nonhydrolyzable purine diphosphate mimic was synthesized. A modular synthetic protocol was developed, utilizing 2-amino-6-(methylthio)-4-(trimethylsilyl)nicotinonitrile as the key synthon in the...
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