DC Field | Value | Language |
---|---|---|
dc.contributor.author | Hong, Seunghee | ko |
dc.contributor.author | Kim, Jinhee | ko |
dc.contributor.author | Yun, Sun-Mi | ko |
dc.contributor.author | Lee, Hyunseung | ko |
dc.contributor.author | PARK, YOONSU | ko |
dc.contributor.author | Hong, Soon-Sun | ko |
dc.contributor.author | Hong, Sungwoo | ko |
dc.date.accessioned | 2013-07-18T07:00:29Z | - |
dc.date.available | 2013-07-18T07:00:29Z | - |
dc.date.created | 2013-06-24 | - |
dc.date.created | 2013-06-24 | - |
dc.date.created | 2013-06-24 | - |
dc.date.created | 2013-06-24 | - |
dc.date.issued | 2013-05 | - |
dc.identifier.citation | JOURNAL OF MEDICINAL CHEMISTRY, v.56, no.9, pp.3531 - 3545 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/10203/174046 | - |
dc.description.abstract | The existence of drug resistance caused by mutations in the break-point cluster region-Abelson tyrosine kinase (Bcr-Abl) kinase domain remains a clinical challenge due to limited effective treatment options for chronic myeloid leukemia (CML). Herein we report a novel series of benzothiazole-based inhibitors that are effective against wild-type and T315I mutant Bcr-Abl kinases. The original hit compound, nocodazole, was extensively modified through a structure-based drug design strategy, especially by varying the groups at the C2 and C6 positions of the scaffold. In addition, the introduction of water-solubilizing groups at the terminal ethyl group resulted in enhanced physicochemical properties and potency in cellular inhibition. Several compounds inhibited the kinase activity of both wild-type Bcr-Abl and the T315I mutant with IC50 values in the picomolar range and exhibited good antiproliferative effects on Ba/F3 cell lines transformed with either wild-type or T315I mutant Bcr-Abl. | - |
dc.language | English | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.title | Discovery of New Benzothiazole-Based Inhibitors of Breakpoint Cluster Region-Abelson Kinase Including the T315I Mutant | - |
dc.type | Article | - |
dc.identifier.wosid | 000318892500010 | - |
dc.identifier.scopusid | 2-s2.0-84877706127 | - |
dc.type.rims | ART | - |
dc.citation.volume | 56 | - |
dc.citation.issue | 9 | - |
dc.citation.beginningpage | 3531 | - |
dc.citation.endingpage | 3545 | - |
dc.citation.publicationname | JOURNAL OF MEDICINAL CHEMISTRY | - |
dc.identifier.doi | 10.1021/jm301891t | - |
dc.contributor.localauthor | PARK, YOONSU | - |
dc.contributor.localauthor | Hong, Sungwoo | - |
dc.contributor.nonIdAuthor | Hong, Seunghee | - |
dc.contributor.nonIdAuthor | Kim, Jinhee | - |
dc.contributor.nonIdAuthor | Yun, Sun-Mi | - |
dc.contributor.nonIdAuthor | Lee, Hyunseung | - |
dc.contributor.nonIdAuthor | Hong, Soon-Sun | - |
dc.description.isOpenAccess | N | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordPlus | CHRONIC MYELOID-LEUKEMIA | - |
dc.subject.keywordPlus | BCR-ABL KINASE | - |
dc.subject.keywordPlus | CHRONIC MYELOGENOUS LEUKEMIA | - |
dc.subject.keywordPlus | GATEKEEPER MUTANT | - |
dc.subject.keywordPlus | CRYSTAL-STRUCTURE | - |
dc.subject.keywordPlus | TYROSINE KINASE | - |
dc.subject.keywordPlus | RESISTANCE | - |
dc.subject.keywordPlus | IMATINIB | - |
dc.subject.keywordPlus | MUTATION | - |
dc.subject.keywordPlus | BIOLOGY | - |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.