Discovery of potent HIV-1 protease inhibitors incorporating sulfoximine functionality

Ding Lu, Robert Vince

Research output: Contribution to journalArticlepeer-review

37 Scopus citations


Based on the unique property of sulfoximine and the homodimeric C2 structural symmetry of HIV-1 protease, a novel class of sulfoximine-based pseudosymmetric HIV-1 protease inhibitors was designed and synthesized. The sulfoximine moiety was demonstrated to be important for HIV-1 protease inhibitor potency. The most active stereoisomer (2S,2′S) displays a potency of 2.5 nM (IC50) against HIV-1 protease and an anti-HIV-1 activity of 408 nM (IC50). A possible mode of action is proposed.

Original languageEnglish (US)
Pages (from-to)5614-5619
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
StatePublished - Oct 15 2007


  • C symmetry
  • HIV-1 protease inhibitor
  • Sulfoximine
  • Transition state mimic


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