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Synthesis and SAR studies for the inhibition of TNF-alpha production. Part 2. 2-[3-(Cyclopentyloxy)-4-methoxyphenyl]-substituted-1-isoindolinone derivatives |
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| Authors: | Park Joon Seok Moon Seong Cheol Baik Kyong Up Cho Jae Youl Yoo Eun Sook Byun Young Seok Park Myung Hwan Balk Kyung Up |
| Affiliation: | Institute of Bioscience & Biotechnology, Daewoong Pharm, Ltd, Yongin, Kyunggi-Do, Korea. joonchem@daewoong.co.kr |
| Abstract: | This study describes the synthesis and in vitro evaluation of 2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1-isoindolinone derivatives substituted on benzene moiety of isoindoline ring for the inhibition of TNF-alpha 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-alpha production in LPS-stimulated RAW264.7 cells. |
| Keywords: | 6-Amino-2-[3-(cyclopentyloxy)-4-methoxyphenyl]-1 -isoindolinone TNFα production inhibitor Structure-activity relationships RAW264.7 |
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