Synthesis and HIV-1 integrase inhibitory activities of caffeoylglucosides.
Caffeoylglucosides, which have a glucose ring as a central linker, were synthesized from methyl D-glucosides, and their anti-HIV-1 activities were tested. Among them, four dicaffeoylglucosides (IC50 = 29.1+/-35.1 microM), 6a, 6b, 9b and 10b, showed HIV-1 integrase inhibitory activity as potent as L-chicoric acid.
Kim
S N
SN
Division of Life Sciences, Korea Institute of Science and Technology, Seoul, South Korea.
Lee
J Y
JY
Kim
H J
HJ
Shin
C G
CG
Park
H
H
Lee
Y S
YS
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002109:Caffeic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005960:Glucosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D019686:Lamiaceae / Q000737:chemistry; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry
D019380:Anti-HIV Agents; D002109:Caffeic Acids; D005960:Glucosides; D019428:HIV Integrase Inhibitors; D019427:HIV Integrase