Development of Novel 1,2,3,4-Tetrahydroquinoline Scaffolds as Potent NF-κB Inhibitors and Cytotoxic Agents.
Basic Information
ID: ALA3808340
Journal: ACS Med Chem Lett
Title: Development of Novel 1,2,3,4-Tetrahydroquinoline Scaffolds as Potent NF-κB Inhibitors and Cytotoxic Agents.
Authors: Jo H, Choi M, Kumar AS, Jung Y, Kim S, Yun J, Kang JS, Kim Y, Han SB, Jung JK, Cho J, Lee K, Kwak JH, Lee H.
Abstract: 1,2,3,4-Tetrahydroquinolines have been identified as the most potent inhibitors of LPS-induced NF-κB 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-κB transcriptional activity and the most potent cytotoxicity against all evaluated human cancer cell lines.
CiteXplore: 27096046
DOI: 10.1021/acsmedchemlett.6b00004
Patent ID: ┄