title: Tricyclic HIV integrase inhibitors V. SAR studies on the benzyl moiety.
abstract: SAR studies on the para-fluorobenzyl moiety of tricyclic HIV integrase inhibitors are discussed and lead compounds with potency and PK properties comparable to raltegravir were identified.
authors.affiliation: Gilead Sciences, Inc, Foster City, CA 94404, USA. hjin@gilead.com
authors.forename: Haolun
authors.initials: H
authors.lastname: Jin
authors.forename: Sammy
authors.initials: S
authors.lastname: Metobo
authors.forename: Salman
authors.initials: S
authors.lastname: Jabri
authors.forename: Michael
authors.initials: M
authors.lastname: Mish
authors.forename: Rachael
authors.initials: R
authors.lastname: Lansdown
authors.forename: Xiaowu
authors.initials: X
authors.lastname: Chen
authors.forename: Manuel
authors.initials: M
authors.lastname: Tsiang
authors.forename: Matthew
authors.initials: M
authors.lastname: Wright
authors.forename: Choung U
authors.initials: CU
authors.lastname: Kim
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D001667:Binding, Competitive / Q000502:physiology; D001682:Biological Availability; D002460:Cell Line; D004285:Dogs; D005464:Fluorobenzenes / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D019428:HIV Integrase Inhibitors / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D051381:Rats; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D019380:Anti-HIV Agents; D005464:Fluorobenzenes; D019428:HIV Integrase Inhibitors