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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-415 |
| Subject |
Discovery of Imidazopyridine Derivatives as Type II Inhibitors of the T315I Mutant BCR-ABL-Target |
| Authors |
Ye Ri Han, Doohyun Lee, Chunyoung Im*
New Drug Development Center, Daegu Gyeongbuk Medical Innovation Foundation, Korea
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| Abstract |
Chronic myeloid leukemia (CML) is a type of cancer caused by the translocation between ABL1 gene in chromosome 9 and the BCR gene in chromosome. This translocation leads to the formation of fusion protein BCR-ABL which are constitutively active tyrosine kinase that induces the pathogenesis of CML. Despite the presence of several well-known inhibitors such as imatinib, Bcr-Abl tyrosine-kinase inhibitors are still receiving significant interest due to the tolerance by the T315I mutation. Therefore, it is important to discover new T315I-mutant BCR-ABL-target inhibitors. Here we describe a imidazopyridine-based type II inhibitors which are targeting T315I-mutated BCR-ABL. The compounds showed significant in vitro efficacy against BCR-ABL-T315I as well as BCR-ABL-WT. In addition, pharmacokinetic data and DMPK profile displayed that the several resulting compounds have optimal ADME properties. Thus, the imidazopyridine-based compounds which are synthesized in this study will be further investigated for the development of a new target treatment for CML. |
| E-mail |
yr6588@naver.com |
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123rd General Meeting of the KCS