title: Synthesis and biological evaluation of andrographolide derivatives as potent anti-HIV agents.
abstract: In an attempt to develop potent anti-HIV drugs, 20 andrographolide derivatives were designed, synthesized, and evaluated for their in vitro anti-HIV activity. The screening results revealed that five compounds showed potent anti-HIV activities with therapeutic indices (TI) above 10. The most promising compound 6f shows a significant TI close to 34.07, with the potency to be a new lead.
authors.affiliation: Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, P. R. China.
authors.forename: Chunlei
authors.initials: C
authors.lastname: Tang
authors.forename: Yajuan
authors.initials: Y
authors.lastname: Liu
authors.forename: Bin
authors.initials: B
authors.lastname: Wang
authors.forename: Guolong
authors.initials: G
authors.lastname: Gu
authors.forename: Liumeng
authors.initials: L
authors.lastname: Yang
authors.forename: Yongtang
authors.initials: Y
authors.lastname: Zheng
authors.forename: Hai
authors.initials: H
authors.lastname: Qian
authors.forename: Wenlong
authors.initials: W
authors.lastname: Huang
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D004224:Diterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008826:Microbial Sensitivity Tests / Q000379:methods / Q000706:statistics & numerical data; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D004224:Diterpenes; C030419:andrographolide