Synthesis and HIV-1 integrase inhibition of novel bis- or tetra-coumarin analogues.
Present studies were undertaken on the preparation of synthetic analogues of bis- or tetra-coumarins and their activity against HIV-1 integrase (HIV-1 IN). Among these coumarin analogues, compounds 14, 16 and 18 were found to be potent molecules against HIV-1 IN at IC50 values of 0.96, 0.58, and 0.49 microM, respectively. The results provided a tool for guiding the further design of more potent antiviral agents and for predicting the affinity of related compounds.
Department of Applied Chemistry and Materials Science, Institute of Technology, National Defense University, Ta-shi, Tao-yuan, Taiwan, ROC..
Chih-Chia
CC
Chiang
Jean-François
JF
Mouscadet
Hou-Jen
HJ
Tsai
Chi-Tsan
CT
Liu
Ling-Yih
LY
Hsu
D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology*; D019427:HIV Integrase / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D009841:Oligonucleotides / Q000138:chemical synthesis / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
D003374:Coumarins; D019428:HIV Integrase Inhibitors; D009841:Oligonucleotides; D019427:HIV Integrase