Chemical modification of coumarin dimer and HIV-1 integrase inhibitory activity.
A systematic series of chemically modified coumarin dimmers has been synthesized and tested for their inhibitory activity against HIV-1 integrase. We observed that modified coumarin dimmers containing hydrophobic moiety on the linker display potent inhibitory activities.
Mao
Pili Chih-Min
PC
Department of Pharmacy, Veterans General Hospital Kaohsiung, Taipei, Tawain, ROC.
Mouscadet
Jean-Francois
JF
Leh
Herve
H
Auclair
Christian
C
Hsu
Ling-Yih
LY
D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019281:Dimerization; D019427:HIV Integrase / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D003374:Coumarins; D019428:HIV Integrase Inhibitors; D019427:HIV Integrase