Picomolar inhibitors of HIV-1 reverse transcriptase: Design and crystallography of naphthyl phenyl ethers

Won Gil Lee, Kathleen M. Frey, Ricardo Gallardo-Macias, Krasimir A. Spasov, Mariela Bollini, Karen S. Anderson, William L. Jorgensen

Research output: Contribution to journalArticlepeer-review

20 Scopus citations

Abstract

Catechol diethers that incorporate a 6-cyano-1-naphthyl substituent have been explored as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Promising compounds are reported that show midpicomolar activity against the wild-type virus and sub-20 nM activity against viral variants bearing Tyr181Cys and Lys103Asn mutations in HIV-RT. An X-ray crystal structure at 2.49 Å resolution is also reported for the key compound 6e with HIV-RT.

Original languageEnglish (US)
Pages (from-to)1259-1262
Number of pages4
JournalACS Medicinal Chemistry Letters
Volume5
Issue number11
DOIs
StatePublished - Nov 13 2014

Bibliographical note

Publisher Copyright:
© 2014 American Chemical Society.

Keywords

  • Anti-HIV agents
  • NNRTIs
  • protein crystallography

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