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Development of Novel 1,2,3,4-Tetrahydroquinoline Scaffolds as Potent NF-kappa B Inhibitors and Cytotoxic Agentsopen access
- Authors
- 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
- Issue Date
- Apr-2016
- Publisher
- AMER CHEMICAL SOC
- Keywords
- 1,2,3,4-Tetrahydroquinolines; NF-kappa B inactivation; in vitro cytotoxicity; human cancer cell lines
- Citation
- ACS MEDICINAL CHEMISTRY LETTERS, v.7, no.4, pp 385 - 390
- Pages
- 6
- Indexed
- SCIE
SCOPUS
- Journal Title
- ACS MEDICINAL CHEMISTRY LETTERS
- Volume
- 7
- Number
- 4
- Start Page
- 385
- End Page
- 390
- ISSN
- 1948-5875
- Abstract
- 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.
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