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BIBTEX RIS

Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates

2007; Elsevier BV; Volume: 17; Issue: 24 Linguagem: Inglês

10.1016/j.bmcl.2007.10.038

ISSN

1464-3405

Autores

Richard L. Mackman, Constantine G. Boojamra, Vidya Prasad, Lijun Zhang, Kuei‐Ying Lin, Oleg V. Petrakovsky, Darius Babusis, James Chen, Janet L. Douglas, Deborah Grant, Hon C. Hui, Choung U. Kim, David Y. Markevitch, Jennifer E. Vela, Adrian S. Ray, Tomáš Cihlář,

Tópico(s)

HIV Research and Treatment

Resumo

A series of nucleoside phosphonate reverse transcriptase (RT) inhibitors have been synthesized and their anti-HIV activity and resistance profiles evaluated. The most potent analog [5-(6-amino-purin-9-yl)-2,5-dihydro-furan-2-yloxymethyl]-phosphonic acid (d4AP) demonstrated a HIV EC(50)=2.1 microM, and the most favorable resistance profile against HIV-1 variants with K65R, M184V or multiple thymidine analog mutations in RT.

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