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

Ho Yoo; Jae Yeol Lee; Jang Hyun Park; Bong Young Chung; Yong Sup Lee

doi:10.1016/j.farmac.2003.08.001

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

Farmaco. 2003 Dec;58(12):1243-50. doi: 10.1016/j.farmac.2003.08.001.

Authors

Ho Yoo¹, Jae Yeol Lee, Jang Hyun Park, Bong Young Chung, Yong Sup Lee

Affiliation

¹ Medicinal Chemistry Research Center, Life Sciences Division, Korea Institute of Science & Technology, P.O. Box 131 Cheongryang, Seoul 130-650, South Korea.

PMID: 14630234
DOI: 10.1016/j.farmac.2003.08.001

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= approximately 40 microM) against HIV-1 integrase, while less than the corresponding styrylquinoline compound (I).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzofurans / chemical synthesis*
Benzofurans / pharmacology
HIV Integrase / metabolism*
HIV Integrase Inhibitors / chemical synthesis*
HIV Integrase Inhibitors / pharmacology
Quinolines / chemical synthesis*
Quinolines / pharmacology

Substances

Benzofurans
HIV Integrase Inhibitors
Quinolines
styrylquinoline
HIV Integrase