Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKbeta inhibitors

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dc.contributor.authorC H Park-
dc.contributor.authorC Lee-
dc.contributor.authorJ S Yang-
dc.contributor.authorB Y Joe-
dc.contributor.authorK Chun-
dc.contributor.authorH Kim-
dc.contributor.authorH Y Kim-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorJ I Lee-
dc.contributor.authorM H Kim-
dc.contributor.authorG Han-
dc.date.accessioned2017-04-19T09:55:33Z-
dc.date.available2017-04-19T09:55:33Z-
dc.date.issued2014-
dc.identifier.issn0960-894X-
dc.identifier.uri10.1016/j.bmcl.2014.04.058ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/12140-
dc.description.abstractInactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting analogues had good inhibitory activity against both nitric oxide and TNF-α, which are well-known inflammatory responses generated by activated NF-κB. However, no inhibitory activity against IKKβ was observed with these compounds. The thienopyrimidine-based analogues were subsequently screened for a target kinase, and FLT3, which is a potential target for acute myeloid leukemia (AML), was identified. Thienopyrimidine-based FLT3 inhibitors showed good inhibition profiles against FLT3 under 1 μM. Overall, these compounds represent a promising family of inhibitors for future development of a treatment for AML.-
dc.publisherElsevier-
dc.titleDiscovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKbeta inhibitors-
dc.title.alternativeDiscovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKbeta inhibitors-
dc.typeArticle-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.number12-
dc.citation.endPage2660-
dc.citation.startPage2655-
dc.citation.volume24-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.alternativeName박천호-
dc.contributor.alternativeName이철호-
dc.contributor.alternativeName양지선-
dc.contributor.alternativeName조보영-
dc.contributor.alternativeName천광우-
dc.contributor.alternativeName김현태-
dc.contributor.alternativeName김혜윤-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeName이장익-
dc.contributor.alternativeName김명화-
dc.contributor.alternativeName한균희-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, vol. 24, no. 12, pp. 2655-2660-
dc.identifier.doi10.1016/j.bmcl.2014.04.058-
dc.subject.keywordAcute myeloid leukemia (AML)-
dc.subject.keywordAnti-inflammation-
dc.subject.keywordFLT3-
dc.subject.keywordIKKβ-
dc.subject.keywordThienopyrimidine-
dc.subject.localacute myeloid leukemia-
dc.subject.localAcute myeloid leukemia-
dc.subject.localAcute myeloid leukemia (AML)-
dc.subject.localantiinflammation-
dc.subject.localAntiinflammation-
dc.subject.localanti-inflammation-
dc.subject.localAnti-Inflammation-
dc.subject.localAnti-inflammation-
dc.subject.localFLT3-
dc.subject.localIKKβ-
dc.subject.localThienopyrimidine-
dc.description.journalClassY-
Appears in Collections:
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
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