title: Synthesis and sar studies for the inhibition of tnf-α production. part 2. 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-substituted-1 -isoindolinone derivatives.
abstract: This study describes the synthesis andin vitro evaluation of 2-[3-(cyclopentyloxy)-4-methox-yphenyl]-1-isoindolinone derivatives substituted on benzene moiety of isoindoline ring for the inhibition of TNF-α production. From this study, we have found the 6-C position on isoindolinone ring is an optimal derivatization site. Among the compounds synthesized, 6-amino-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1 -isoindolinone (6) was the most potent in inhibitory activity of TNF-α production in LPS-stimulated RAW264.7 cells.
authors: Institute of Bioscience & Biotechnology, Daewoong Pharm. Co., Ltd., 449-814, Yongin, Kyunggi-Do, Korea. joonchem@daewoong.co.kr.
authors: Joon Seok
authors: JS
authors: Park
authors: Institute of Bioscience & Biotechnology, Daewoong Pharm. Co., Ltd., 449-814, Yongin, Kyunggi-Do, Korea.
authors: Seong Cheol
authors: SC
authors: Moon
authors: Institute of Bioscience & Biotechnology, Daewoong Pharm. Co., Ltd., 449-814, Yongin, Kyunggi-Do, Korea.
authors: Kyung Up
authors: KU
authors: Baik
authors: Institute of Bioscience & Biotechnology, Daewoong Pharm. Co., Ltd., 449-814, Yongin, Kyunggi-Do, Korea.
authors: Jae Youl
authors: JY
authors: Cho
authors: Institute of Bioscience & Biotechnology, Daewoong Pharm. Co., Ltd., 449-814, Yongin, Kyunggi-Do, Korea.
authors: Eun Sook
authors: ES
authors: Yoo
authors: Institute of Bioscience & Biotechnology, Daewoong Pharm. Co., Ltd., 449-814, Yongin, Kyunggi-Do, Korea.
authors: Young Seok
authors: YS
authors: Byun
authors: Institute of Bioscience & Biotechnology, Daewoong Pharm. Co., Ltd., 449-814, Yongin, Kyunggi-Do, Korea.
authors: Myung Hwan
authors: MH
authors: Park
keywords: 6-Amino-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1 -isoindolinone; RAW264.7; Structure-activity relationships; TNFα production inhibitor