Structure-activity relationship of indoline-2-carboxylic acid N-(substituted)phenylamide derivatives.
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.
Kwak
Jae-Hwan
JH
Department of Pharmacy, Chungbuk National University, Chungbuk, Republic of Korea.
Kim
Yoseob
Y
Park
Hyunjeong
H
Jang
Jae-Yong
JY
Lee
Keun Kuk
KK
Yi
Wonhui
W
Kwak
Jeong-Ah
JA
Park
Song-Gyu
SG
Kim
Hwanmook
H
Lee
Kiho
K
Kang
Jong Soon
JS
Han
Sang-Bae
SB
Hwang
Bang Yeon
BY
Hong
Jin Tae
JT
Jung
Jae-Kyung
JK
Kim
Youngsoo
Y
Cho
Jungsook
J
Lee
Heesoon
H
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D001596:Benzylamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D002839:Chromans / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D016328:NF-kappa B / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D001596:Benzylamines; D002839:Chromans; D007211:Indoles; D016328:NF-kappa B; C057812:indoline; C030796:benzylamine