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

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2016 Apr 21

PMID 27096046

Citations 2

Authors

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

Affiliations

Soon will be listed here.

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.

Citing Articles

Ground State Generation and Cyclization of Aminium Radicals in the Formation of Tetrahydroquinolines.

Pratley C, Fenner S, Murphy J Org Lett. 2024; 26(6):1287-1292.

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Suppression of Pax3-MITF-M Axis Protects from UVB-Induced Skin Pigmentation by Tetrahydroquinoline Carboxamide.

Choi Y, Kim G, Kim S, Maeng J, Lee H, Han S Int J Mol Sci. 2020; 21(24).

PMID: 33348800 PMC: 7766340. DOI: 10.3390/ijms21249631.

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