Development of Novel 1,2,3,4-Tetrahydroquinoline Scaffolds as Potent NF-kappa B Inhibitors and Cytotoxic Agents

作者：Jo Hyeju; Choi Minho; Kumar Areyalli Sateesh; Jung Yeongeun; Kim Sangeun; Yun Jieun; Kang Jong Soon; Kim Youngsoo; Han Sang bae; Jung Jae Kyung; Cho Jungsook; Lee Kiho; Kwak Jae Hwan; Lee Heesoon^*

来源：ACS Medicinal Chemistry Letters, 2016, 7(4): 385-390.

DOI：10.1021/acsmedchemlett.6b00004

• 1,2,3,4-Tetrahydroquinolines
• NF-kappa B inactivation
• in vitro cytotoxicity
• human cancer cell lines

1,2,3,4-Tetrahydroquinolines have been identified as the most potent inhibitors of LPS-induced NF-kappa B transcriptional activity. To discover new molecules of this class with excellent activities, we designed and synthesized a series of novel derivatives of 1,2,3,4-tetrahydroquinolines (4a-g, 5a-h, 6a-h, and 7a-h) and bioevaluated their in vitro activity against human cancer cell lines (NCI-H23, ACHN, MDA-MB-231, PC-3, NUGC-3, and HCT 15). Among all synthesized scaffolds, 6g exhibited the most potent inhibition (53 times that of a reference compound) of LPS-induced NF-kappa B transcriptional activity and the most potent cytotoxicity against all evaluated human cancer cell lines.

• 出版日期2016-4