Synthesis of styrylbenzofuran derivatives as styrylquinoline analogues for HIV-1 integrase inhibitor.
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= approximately 40 microM) against HIV-1 integrase, while less than the corresponding styrylquinoline compound (I).
Yoo
Ho
H
Medicinal Chemistry Research Center, Life Sciences Division, Korea Institute of Science & Technology, P.O. Box 131 Cheongryang, Seoul 130-650, South Korea.
Lee
Jae Yeol
JY
Park
Jang Hyun
JH
Chung
Bong Young
BY
Lee
Yong Sup
YS
D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology
D001572:Benzofurans; D019428:HIV Integrase Inhibitors; D011804:Quinolines; C481600:styrylquinoline; D019427:HIV Integrase