Ippolito, Joseph A.; Niu, Haichan; Bertoletti, Nicole; Carter, Zachary J.; Jin, Shengyan; Spasov, Krasimir A.; Cisneros, Jose A.; Valhondo, Margarita; Cutrona, Kara J.; Anderson, Karen S.; Jorgensen, William L. published the artcile< Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead>, SDS of cas: 16766-30-6, the main research area is covalent inhibitor HIV1 RT fluorosulfate warhead preparation.
Covalent inhibitors of wild-type HIV-1 reverse transcriptase (CRTIs) are reported. Three compounds derived from catechol diether non-nucleoside inhibitors (NNRTIs) with addition of a fluorosulfate warhead are demonstrated to covalently modify Tyr181 of HIV-RT. X-ray crystal structures for complexes of the CRTIs with the enzyme are provided, which fully demonstrate the covalent attachment, and confirmation is provided by appropriate mass shifts in ESI-TOF mass spectra. The three CRTIs and six noncovalent analogs are found to be potent inhibitors with both IC50 values for in vitro inhibition of WT RT and EC50 values for cytopathic protection of HIV-1-infected human T-cells in the 5-320 nM range.
ACS Medicinal Chemistry Letters published new progress about Anti-HIV agents (anti-HIV-1 agents, Anti-HIV-1 drugs). 16766-30-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO2, SDS of cas: 16766-30-6.
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