Design, synthesis, and biological evaluation of potent 1,2,3,4-tetrahydroisoquinoline derivatives as anticancer agents targeting NF-κB signaling pathway

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dc.contributor.authorS Sim-
dc.contributor.authorS Lee-
dc.contributor.authorS Ko-
dc.contributor.authorB PP Bui-
dc.contributor.authorP L Nguyen-
dc.contributor.authorJ Cho-
dc.contributor.authorK Lee-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorJ K Jung-
dc.contributor.authorH Lee-
dc.date.accessioned2021-09-13T15:30:19Z-
dc.date.available2021-09-13T15:30:19Z-
dc.date.issued2021-
dc.identifier.issn09680896-
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/24720-
dc.description.abstractThe multifunctional transcription factor, nuclear factor-κB (NF-κB), is broadly involved in multiple human diseases, such as cancer and chronic inflammation, through abnormal modulations of the NF-κB signaling cascades. In patients with several types of cancer diseases, NF-κB is excessively activated, which could result in the stimulation of proliferation and/or suppression of apoptosis. Herein, we present a new series of 1,2,3,4-tetrahydroisoquinoline derivatives with good anticancer activities against various human cancer cell lines, which are rationally designed based on our novel NF-κB inhibitors. The SAR studies demonstrated that compound 5d with a methoxy group at the R3 position exhibits the most anti-proliferative activity with GI50 values, ranging 1.591 to 2.281 μM. Similar to KL-1156, the compound 5d (HSR1304) blocked NF-κB nuclear translocation step in LPS-stimulated MDA-MB-231 cells, probably leading to cytotoxic potency against tumor cells. Together with known potent NF-κB inhibitors containing diverse core heterocyclic moieties, the 1,2,3,4-tetrahydroisoquinoline derivatives can provide structural diversity, enhancing a potential for the development of a novel class of anticancer drugs.-
dc.publisherElsevier-
dc.titleDesign, synthesis, and biological evaluation of potent 1,2,3,4-tetrahydroisoquinoline derivatives as anticancer agents targeting NF-κB signaling pathway-
dc.title.alternativeDesign, synthesis, and biological evaluation of potent 1,2,3,4-tetrahydroisoquinoline derivatives as anticancer agents targeting NF-κB signaling pathway-
dc.typeArticle-
dc.citation.titleBioorganic & Medicinal Chemistry-
dc.citation.number0-
dc.citation.endPage116371-
dc.citation.startPage116371-
dc.citation.volume46-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.alternativeName심성락-
dc.contributor.alternativeName이수미-
dc.contributor.alternativeName고승균-
dc.contributor.alternativeNameBui-
dc.contributor.alternativeNameNguyen-
dc.contributor.alternativeName조정숙-
dc.contributor.alternativeName이기호-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeName정재경-
dc.contributor.alternativeName이희순-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry, vol. 46, pp. 116371-116371-
dc.identifier.doi10.1016/j.bmc.2021.116371-
dc.subject.keywordNF-κB signaling-
dc.subject.keywordAnticancer activity-
dc.subject.keyword1,2,3,4-Tetrahydroisoquinoline-
dc.subject.keywordHuman cancer cell lines-
dc.subject.keywordNF-κB nuclear translocation-
dc.subject.localAnticancer activity-
dc.description.journalClassY-
Appears in Collections:
Ochang Branch Institute > Division of Bioinfrastructure > Laboratory Animal Resource Center > 1. Journal Articles
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