title: HIV-1 integrase inhibition of biscoumarin analogues.
abstract: Nineteen biscoumarins bearing free and modified hydroxyl substituents at benzoyloxyphenyl linker have been synthesized by multiple step synthesis. Among these biscoumarins, thirteen were found to be active molecules against HIV-1 integrase (HIV-1 IN). The structure-activity relationship of the nineteen compounds on HIV IN may be useful for the design of potent therapeutic agents.
authors.affiliation: School of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan, ROC.
authors.forename: Chang-Xiao
authors.initials: CX
authors.lastname: Su
authors.forename: Jean-Francois
authors.initials: JF
authors.lastname: Mouscadet
authors.forename: Chih-Chia
authors.initials: CC
authors.lastname: Chiang
authors.forename: Hou-Jen
authors.initials: HJ
authors.lastname: Tsai
authors.forename: Ling-Yih
authors.initials: LY
authors.lastname: Hsu
mesh_terms: D000107:Acetylation; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology*; D006868:Hydrolysis; D006900:Hydroxylation; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D009841:Oligonucleotides / Q000138:chemical synthesis / Q000494:pharmacology; D010636:Phenols / Q000737:chemistry; D059808:Polyphenols; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013329:Structure-Activity Relationship; D008063:Thioctic Acid / Q000737:chemistry
chemical_list: D003374:Coumarins; D005419:Flavonoids; D019428:HIV Integrase Inhibitors; D007202:Indicators and Reagents; D009841:Oligonucleotides; D010636:Phenols; D059808:Polyphenols; D008063:Thioctic Acid