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

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• 作者：Hyeju Jo ; Minho Choi ; Arepalli Sateesh Kumar ; Yeongeun Jung ; Sangeun Kim ; Jieun Yun ; Jong-Soon Kang ; Youngsoo Kim ; Sang-bae Han ; Jae-Kyung Jung ; Jungsook Cho ; Kiho Lee ; Jae-Hwan Kwak ; Heesoon Lee
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：April 14, 2016
• 年：2016
• 卷：7
• 期：4
• 页码：385-390
• 全文大小：359K
• 年卷期：0
• ISSN：1948-5875

文摘

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.