1. Academic Validation
  2. Structure-activity relationship of indoline-2-carboxylic acid N-(substituted)phenylamide derivatives

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

  • Bioorg Med Chem Lett. 2010 Aug 1;20(15):4620-3. doi: 10.1016/j.bmcl.2010.06.004.
Jae-Hwan Kwak 1 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
Affiliations

Affiliation

  • 1 Department of Pharmacy, Chungbuk National University, Chungbuk, Republic of Korea.
Abstract

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.

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