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.
Chiang
Chih-Chia
CC
Department of Applied Chemistry and Materials Science, Institute of Technology, National Defense University, Ta-shi, Tao-yuan, Taiwan, ROC..
Mouscadet
Jean-François
JF
Tsai
Hou-Jen
HJ
Liu
Chi-Tsan
CT
Hsu
Ling-Yih
LY
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