Structure–activity relationship of indoline-2-carboxylic acid N-(substituted)phenylamide derivatives

✍ Scribed by Jae-Hwan Kwak; Yoseob Kim; Hyunjeong Park; Jae-Yong Jang; Keun Kuk Lee; Wonhui Yi; Jeong-Ah Kwak; Song-Gyu Park; Hwanmook Kim; Kiho Lee; Jong Soon Kang; Sang-Bae Han; Bang Yeon Hwang; Jin Tae Hong; Jae-Kyung Jung; Youngsoo Kim; Jungsook Cho; Heesoon Lee

• Book ID: 104004490
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 251 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.06.004

✦ Synopsis

Chroman derivatives exhibited potent inhibitory activity of NF-kappaB. For SAR, the chroman scaffold was modified with an indoline moiety. A series of indoline-2-carboxylic acid N-(substituted)phenylamide derivatives were synthesized to explore their inhibitory activities of NF-kappaB and they were also evaluated for cytotoxicity against various cancer cell lines. Since intermediates with Boc showed outstanding results, various substituents in place of the Boc group were introduced additionally and these compounds were also evaluated for SAR.