DC Field | Value | Language |
---|---|---|
dc.contributor.author | C H Park | - |
dc.contributor.author | C Lee | - |
dc.contributor.author | J S Yang | - |
dc.contributor.author | B Y Joe | - |
dc.contributor.author | K Chun | - |
dc.contributor.author | H Kim | - |
dc.contributor.author | H Y Kim | - |
dc.contributor.author | Jong Soon Kang | - |
dc.contributor.author | J I Lee | - |
dc.contributor.author | M H Kim | - |
dc.contributor.author | G Han | - |
dc.date.accessioned | 2017-04-19T09:55:33Z | - |
dc.date.available | 2017-04-19T09:55:33Z | - |
dc.date.issued | 2014 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | 10.1016/j.bmcl.2014.04.058 | ko |
dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/12140 | - |
dc.description.abstract | Inactivation 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.publisher | Elsevier | - |
dc.title | Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKbeta inhibitors | - |
dc.title.alternative | Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKbeta inhibitors | - |
dc.type | Article | - |
dc.citation.title | Bioorganic & Medicinal Chemistry Letters | - |
dc.citation.number | 12 | - |
dc.citation.endPage | 2660 | - |
dc.citation.startPage | 2655 | - |
dc.citation.volume | 24 | - |
dc.contributor.affiliatedAuthor | Jong Soon Kang | - |
dc.contributor.alternativeName | 박천호 | - |
dc.contributor.alternativeName | 이철호 | - |
dc.contributor.alternativeName | 양지선 | - |
dc.contributor.alternativeName | 조보영 | - |
dc.contributor.alternativeName | 천광우 | - |
dc.contributor.alternativeName | 김현태 | - |
dc.contributor.alternativeName | 김혜윤 | - |
dc.contributor.alternativeName | 강종순 | - |
dc.contributor.alternativeName | 이장익 | - |
dc.contributor.alternativeName | 김명화 | - |
dc.contributor.alternativeName | 한균희 | - |
dc.identifier.bibliographicCitation | Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 12, pp. 2655-2660 | - |
dc.identifier.doi | 10.1016/j.bmcl.2014.04.058 | - |
dc.subject.keyword | Acute myeloid leukemia (AML) | - |
dc.subject.keyword | Anti-inflammation | - |
dc.subject.keyword | FLT3 | - |
dc.subject.keyword | IKKβ | - |
dc.subject.keyword | Thienopyrimidine | - |
dc.subject.local | acute myeloid leukemia | - |
dc.subject.local | Acute myeloid leukemia | - |
dc.subject.local | Acute myeloid leukemia (AML) | - |
dc.subject.local | antiinflammation | - |
dc.subject.local | Antiinflammation | - |
dc.subject.local | anti-inflammation | - |
dc.subject.local | Anti-Inflammation | - |
dc.subject.local | Anti-inflammation | - |
dc.subject.local | FLT3 | - |
dc.subject.local | IKKβ | - |
dc.subject.local | Thienopyrimidine | - |
dc.description.journalClass | Y | - |
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