Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents

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dc.contributor.authorJ S Yang-
dc.contributor.authorC H Park-
dc.contributor.authorC Lee-
dc.contributor.authorH Kim-
dc.contributor.authorC Oh-
dc.contributor.authorY Choi-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorJi Eun Yun-
dc.contributor.authorJ H Jeong-
dc.contributor.authorM H Kim-
dc.contributor.authorG Han-
dc.date.accessioned2017-04-19T09:55:24Z-
dc.date.available2017-04-19T09:55:24Z-
dc.date.issued2014-
dc.identifier.issn02235234-
dc.identifier.uri10.1016/j.ejmech.2014.08.001ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/12113-
dc.description.abstractThe most common mutations in acute myeloid leukemia (AML) are those that cause the activation of FMS-like tyrosine kinase 3 (FLT3). Therefore, FLT3 is regarded as a potential target for the treatment of AML. A novel series of thieno[2,3-d]pyrimidine-based analogs was designed and synthesized as FLT3 inhibitors. All synthesized compounds were assayed for the tyrosine kinase activity of FLT3 and growth inhibitory activity in four human leukemia cell lines (THP1, MV4-11, K562, and HL-60). Among these compounds, compound 17a, which possesses relatively short and simple substituents at the C6 position of thieno[2,3-d]pyrimidine, emerged as the most promising anti-leukemic agent. Compound 17a exhibited potent inhibition of FLT3-positive leukemic cell growth and of the FLT3 D835Y kinase; such inhibition is required for the successful treatment of AML. The data supports the further investigation of this class of compounds as potential anti-leukemic agents.-
dc.publisherElsevier-
dc.titleSynthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents-
dc.title.alternativeSynthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents-
dc.typeArticle-
dc.citation.titleEuropean Journal of Medicinal Chemistry-
dc.citation.numberC-
dc.citation.endPage407-
dc.citation.startPage399-
dc.citation.volume85-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.alternativeName양지선-
dc.contributor.alternativeName박춘호-
dc.contributor.alternativeName이철호-
dc.contributor.alternativeName김환-
dc.contributor.alternativeName오창목-
dc.contributor.alternativeName최예주-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeName윤지은-
dc.contributor.alternativeName정진현-
dc.contributor.alternativeName김명화-
dc.contributor.alternativeName한균희-
dc.identifier.bibliographicCitationEuropean Journal of Medicinal Chemistry, vol. 85, no. C, pp. 399-407-
dc.identifier.doi10.1016/j.ejmech.2014.08.001-
dc.subject.keywordAcute myeloid leukemia (AML)-
dc.subject.keywordD835Y-
dc.subject.keywordFMS-like tyrosine kinase 3 (FLT3)-
dc.subject.keywordInternal tandem duplications (ITD)-
dc.subject.keywordThieno[2,3-d]pyrimidine-
dc.subject.localAcute myeloid leukemia (AML)-
dc.subject.localAcute myeloid leukemia-
dc.subject.localD835Y-
dc.subject.localFMS-like tyrosine kinase 3 (FLT3)-
dc.subject.localInternal tandem duplications (ITD)-
dc.subject.localThieno[2,3-d]pyrimidine-
dc.description.journalClassY-
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Ochang Branch Institute > Division of Bioinfrastructure > Laboratory Animal Resource Center > 1. Journal Articles
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