DC Field | Value | Language |
---|---|---|
dc.contributor.author | S Sim | - |
dc.contributor.author | S Lee | - |
dc.contributor.author | S Ko | - |
dc.contributor.author | B PP Bui | - |
dc.contributor.author | P L Nguyen | - |
dc.contributor.author | J Cho | - |
dc.contributor.author | K Lee | - |
dc.contributor.author | Jong Soon Kang | - |
dc.contributor.author | J K Jung | - |
dc.contributor.author | H Lee | - |
dc.date.accessioned | 2021-09-13T15:30:19Z | - |
dc.date.available | 2021-09-13T15:30:19Z | - |
dc.date.issued | 2021 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/24720 | - |
dc.description.abstract | The 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.publisher | Elsevier | - |
dc.title | Design, synthesis, and biological evaluation of potent 1,2,3,4-tetrahydroisoquinoline derivatives as anticancer agents targeting NF-κB signaling pathway | - |
dc.title.alternative | Design, synthesis, and biological evaluation of potent 1,2,3,4-tetrahydroisoquinoline derivatives as anticancer agents targeting NF-κB signaling pathway | - |
dc.type | Article | - |
dc.citation.title | Bioorganic & Medicinal Chemistry | - |
dc.citation.number | 0 | - |
dc.citation.endPage | 116371 | - |
dc.citation.startPage | 116371 | - |
dc.citation.volume | 46 | - |
dc.contributor.affiliatedAuthor | Jong Soon Kang | - |
dc.contributor.alternativeName | 심성락 | - |
dc.contributor.alternativeName | 이수미 | - |
dc.contributor.alternativeName | 고승균 | - |
dc.contributor.alternativeName | Bui | - |
dc.contributor.alternativeName | Nguyen | - |
dc.contributor.alternativeName | 조정숙 | - |
dc.contributor.alternativeName | 이기호 | - |
dc.contributor.alternativeName | 강종순 | - |
dc.contributor.alternativeName | 정재경 | - |
dc.contributor.alternativeName | 이희순 | - |
dc.identifier.bibliographicCitation | Bioorganic & Medicinal Chemistry, vol. 46, pp. 116371-116371 | - |
dc.identifier.doi | 10.1016/j.bmc.2021.116371 | - |
dc.subject.keyword | NF-κB signaling | - |
dc.subject.keyword | Anticancer activity | - |
dc.subject.keyword | 1,2,3,4-Tetrahydroisoquinoline | - |
dc.subject.keyword | Human cancer cell lines | - |
dc.subject.keyword | NF-κB nuclear translocation | - |
dc.subject.local | NF-κB signaling | - |
dc.subject.local | Anti-cancer activity | - |
dc.subject.local | Anticancer activity | - |
dc.subject.local | anticancer activity | - |
dc.subject.local | 1,2,3,4-Tetrahydroisoquinoline | - |
dc.subject.local | Human cancer cell line | - |
dc.subject.local | human cancer cell lines | - |
dc.subject.local | Human cancer cell lines | - |
dc.subject.local | NF-κB nuclear translocation | - |
dc.description.journalClass | Y | - |
There are no files associated with this item.
Items in OpenAccess@KRIBB are protected by copyright, with all rights reserved, unless otherwise indicated.