A novel 3-arylethynyl-substituted pyrido[2,3,-b]pyrazine derivatives and pharmacophore model as Wnt2/beta-catenin pathway inhibitors in non-small-cell lung cancer cell lines
DC Field | Value | Language |
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dc.contributor.author | Gong, Young-Dae | - |
dc.contributor.author | Dong, Mi-Sook | - |
dc.contributor.author | Lee, Sang-Bum | - |
dc.contributor.author | Kim, Nayeon | - |
dc.contributor.author | Bae, Mi-Seon | - |
dc.contributor.author | Kang, Nam-Sook | - |
dc.date.accessioned | 2021-09-07T08:20:18Z | - |
dc.date.available | 2021-09-07T08:20:18Z | - |
dc.date.created | 2021-06-19 | - |
dc.date.issued | 2011-09-15 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/111578 | - |
dc.description.abstract | We developed Wnt/beta-catenin inhibitors by identifying 13 number of 3-arylethynyl-substituted pyrido[2,3,-b] pyrazine derivatives that were able to inhibit the Wnt/b-catenin signal pathway and cancer cell proliferation. In the optimization process, a series of 2,3,6-trisubstituted pyrido[2,3,-b] pyrazine core skeletons showed were shown to higher activity than 2,3,6-trisubstituted quinoxaline's and thus hold promise for use as potential small-molecule inhibitors of the Wnt/beta-catenin signal pathway in non-small-cell lung cancer cell (NSCLC) lines. And we have studied the pharmacophore mapping for compound 954, which presented the highest activity with a fit value of 2.81. The pharmacophore mapping for the compounds including 954, pyrido[2,3,-b] pyrazine core had hydrogen-bond acceptor site and hydrophobic center roles. (C) 2011 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | SOLID-PHASE SYNTHESIS | - |
dc.subject | BETA-CATENIN | - |
dc.subject | PARALLEL SYNTHESIS | - |
dc.subject | GASTRIC-CANCER | - |
dc.subject | WNT | - |
dc.subject | ACTIVATION | - |
dc.subject | EXPRESSION | - |
dc.subject | MUTATIONS | - |
dc.subject | LIBRARY | - |
dc.subject | LINKER | - |
dc.title | A novel 3-arylethynyl-substituted pyrido[2,3,-b]pyrazine derivatives and pharmacophore model as Wnt2/beta-catenin pathway inhibitors in non-small-cell lung cancer cell lines | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Dong, Mi-Sook | - |
dc.identifier.doi | 10.1016/j.bmc.2011.07.028 | - |
dc.identifier.scopusid | 2-s2.0-80052592243 | - |
dc.identifier.wosid | 000294711100036 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY, v.19, no.18, pp.5639 - 5647 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.citation.volume | 19 | - |
dc.citation.number | 18 | - |
dc.citation.startPage | 5639 | - |
dc.citation.endPage | 5647 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | SOLID-PHASE SYNTHESIS | - |
dc.subject.keywordPlus | BETA-CATENIN | - |
dc.subject.keywordPlus | PARALLEL SYNTHESIS | - |
dc.subject.keywordPlus | GASTRIC-CANCER | - |
dc.subject.keywordPlus | WNT | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | MUTATIONS | - |
dc.subject.keywordPlus | LIBRARY | - |
dc.subject.keywordPlus | LINKER | - |
dc.subject.keywordAuthor | Wnt2 | - |
dc.subject.keywordAuthor | beta-Catenin | - |
dc.subject.keywordAuthor | Pyrido[ 2,3,-b]pyrazines | - |
dc.subject.keywordAuthor | Inhibitors | - |
dc.subject.keywordAuthor | Anti-cancer | - |
dc.subject.keywordAuthor | Pharmacophore | - |
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