Synthesis of styrylbenzofuran derivatives as styrylquinoline analogues for HIV-1 integrase inhibitor

Authors
Yoo, H.Lee, J.Y.Park, J.H.Chung, B.Y.Lee, Y.S.
Issue Date
2003-12
Publisher
Elsevier Masson SAS
Citation
Farmaco, v.58, no.12, pp.1243 - 1250
Abstract
A series of styrylbenzofuran derivatives (8a-i) as styrylquinoline isosters were efficiently prepared by Wittig reaction and evaluated for inhibitory activity against HIV-1 integrase. In this series, compounds 8g, 8h and 8i containing a free catechol ring showed moderate inhibitory activities (IC50=∼40 μM) against HIV-1 integrase, while less than the corresponding styrylquinoline compound (I). ? 2003 ?ditions scientifiques et m?dicales Elsevier SAS. All rights reserved.
Keywords
7 hydroxy 2 [2 (3,4 dihydroxyphenyl)ethenyl] 6 benzofuran carboxylic acid; 7 hydroxy 2 [2 (4 hydroxyphenyl)ethynyl] 6 benzofuran carboxylic acid; 7 methoxy 2 [2 (4 hydroxyphenyl)ethenyl] 6 benzofuran carboxylic acid; benzofuran derivative; integrase inhibitor; methyl 7 hydroxy 2 [2 (3,4 dihydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 hydroxy 2 [2 (4 hydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (3,4 dihydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (3,4 dimethoxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (4 hydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (4 methoxyphenyl)ethenyl] 6 benzofuran carboxylate; quinoline derivative; unclassified drug; article; drug activity; drug screening; drug structure; drug synthesis; enzyme inhibition; Human immunodeficiency virus 1; IC 50; nonhuman; Wittig reaction; 7 hydroxy 2 [2 (3,4 dihydroxyphenyl)ethenyl] 6 benzofuran carboxylic acid; 7 hydroxy 2 [2 (4 hydroxyphenyl)ethynyl] 6 benzofuran carboxylic acid; 7 methoxy 2 [2 (4 hydroxyphenyl)ethenyl] 6 benzofuran carboxylic acid; benzofuran derivative; integrase inhibitor; methyl 7 hydroxy 2 [2 (3,4 dihydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 hydroxy 2 [2 (4 hydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (3,4 dihydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (3,4 dimethoxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (4 hydroxyphenyl)ethenyl] 6 benzofuran carboxylate; methyl 7 methoxy 2 [2 (4 methoxyphenyl)ethenyl] 6 benzofuran carboxylate; quinoline derivative; unclassified drug; article; drug activity; drug screening; drug structure; drug synthesis; enzyme inhibition; Human immunodeficiency virus 1; IC 50; nonhuman; Wittig reaction; AIDS; HIV; Integrase inhibitor; Styrylbenzofuran; Wittig reaction
ISSN
0014-827X
URI
https://pubs.kist.re.kr/handle/201004/138068
DOI
10.1016/j.farmac.2003.08.001
Appears in Collections:
KIST Article > 2003
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