Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C-2 and C-6 positions
DC Field | Value | Language |
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dc.contributor.author | Oh, Changmok | - |
dc.contributor.author | Kim, Hyuntae | - |
dc.contributor.author | Kang, Jong Soon | - |
dc.contributor.author | Yun, Jieun | - |
dc.contributor.author | Sim, Jaejun | - |
dc.contributor.author | Kim, Hwan-Mook | - |
dc.contributor.author | Han, Gyoonhee | - |
dc.date.available | 2020-02-27T19:43:39Z | - |
dc.date.created | 2020-02-07 | - |
dc.date.issued | 2017-02-01 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/6403 | - |
dc.description.abstract | Acute myeloid leukemia (AML) is a clonal disorder of hematopoietic progenitor cell. In AML, a mutation in FLT3 is commonly occurs and is associated with poor prognosis. We have previously reported that thieno [2,3-d]pyrimidine derivative compound 1 exhibited better antiproliferative activity against MV4-11 cells which harbor mutant FLT3 than AC220, which is a well-known FLT3 inhibitor, and has good microsomal stability. However, compound 1 had poor solubility. We then carried out further structural modification at the C-2 and the C-6 positions of thieno[2,3-d]pyrimidine scaffold. Compound 13b, which possesses a thiazole moiety at the C-2 position, exhibited better antiproliferative activity than compound 1 and showed increased solubility and moderate microsomal stability. These results indicate that compound 13b could be a promising potential FLT inhibitor for AML chemotherapy. (C) 2016 Elsevier Ltd. All rights reserved. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.subject | ACUTE MYELOID-LEUKEMIA | - |
dc.subject | INTERNAL TANDEM DUPLICATION | - |
dc.subject | PROGNOSTIC-SIGNIFICANCE | - |
dc.subject | MUTATIONS | - |
dc.subject | CANCER | - |
dc.title | Synthetic strategy for increasing solubility of potential FLT3 inhibitor thieno[2,3-d]pyrimidine derivatives through structural modifications at the C-2 and C-6 positions | - |
dc.type | Article | - |
dc.type.rims | ART | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000392900600023 | - |
dc.identifier.doi | 10.1016/j.bmcl.2016.12.034 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.3, pp.496 - 500 | - |
dc.identifier.scopusid | 2-s2.0-85009067207 | - |
dc.citation.endPage | 500 | - |
dc.citation.startPage | 496 | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 27 | - |
dc.citation.number | 3 | - |
dc.contributor.affiliatedAuthor | Sim, Jaejun | - |
dc.contributor.affiliatedAuthor | Kim, Hwan-Mook | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | FLT3 | - |
dc.subject.keywordAuthor | Thieno[2,3-d]pyrimidine | - |
dc.subject.keywordAuthor | Acute myeloid leukemia (AML) | - |
dc.subject.keywordAuthor | Solubility | - |
dc.subject.keywordPlus | ACUTE MYELOID-LEUKEMIA | - |
dc.subject.keywordPlus | INTERNAL TANDEM DUPLICATION | - |
dc.subject.keywordPlus | PROGNOSTIC-SIGNIFICANCE | - |
dc.subject.keywordPlus | MUTATIONS | - |
dc.subject.keywordPlus | CANCER | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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