title: Indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors.
abstract: Compound 1 (VEC-5) was identified as a potent small-molecular HIV-1 viron infectivity factor inhibitor that targets the viron infectivity factor-ElonginC interaction. A structure-activity relationship study was carried out to develop compounds with improved efficacy against HIV-1 and 49 indolizine derivatives of three categories were designed and synthesized. We found that five compounds exhibited promising anti-HIV-1 activity, and the most active compound 2g had an IC50 value of 11.0 μm. These results provide new information to develop highly potent small-molecule HIV-1 viron infectivity factor inhibitors.
authors: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors: Wenlin
authors: W
authors: Huang
authors: Tao
authors: T
authors: Zuo
authors: Xiao
authors: X
authors: Luo
authors: Hongwei
authors: H
authors: Jin
authors: Zhenming
authors: Z
authors: Liu
authors: Zhenjun
authors: Z
authors: Yang
authors: Xianghui
authors: X
authors: Yu
authors: Liangren
authors: L
authors: Zhang
authors: Lihe
authors: L
authors: Zhang
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D000075065:Elongin; D015497:HIV-1 / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D007212:Indolizines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000037:antagonists & inhibitors / Q000378:metabolism*; D054320:vif Gene Products, Human Immunodeficiency Virus / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D019380:Anti-HIV Agents; D000075065:Elongin; D007212:Indolizines; D014157:Transcription Factors; C585391:ethyl 3-(2-naphthoyl)-7-isonicotinoylindolizine-1-carboxylate; D054320:vif Gene Products, Human Immunodeficiency Virus; C035094:indolizine