HIV-1 integrase inhibition of biscoumarin analogues.
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.
Su
Chang-Xiao
CX
School of Pharmacy, National Defense Medical Center, Taipei 114, Taiwan, ROC.
Mouscadet
Jean-Francois
JF
Chiang
Chih-Chia
CC
Tsai
Hou-Jen
HJ
Hsu
Ling-Yih
LY
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
D003374:Coumarins; D005419:Flavonoids; D019428:HIV Integrase Inhibitors; D007202:Indicators and Reagents; D009841:Oligonucleotides; D010636:Phenols; D059808:Polyphenols; D008063:Thioctic Acid