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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-373 |
| Subject |
Design, Synthesis, and Enzyme Inhibitory Activities against AXL and ACK1 of Novel Aminopyrimidine Derivatives |
| Authors |
Juri Suh, Jongseung Kim, Kyung Ho Yoo1,*
Department of Chemistry, Korea University, Korea
1Chemical Kinomics Research Center, Korea Institute of Science and Technology, Korea
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| Abstract |
AXL is a receptor tyrosine kinase involved in the growth, differentiation, survival, and motility of many different cell types. AXL has been implicated as a cancer driver and correlated with poor survival in numerous aggressive tumors including TNBC, AML, NSCLC, pancreatic cancer, and ovarian cancer. The emergence of ACK1 as an oncogenic kinase has uncovered novel mechanisms by which tyrosine kinase signaling promotes cancer progression. The ACK1 tyrosine kinase is aberrantly activated, amplified, or mutated in many types of human cancers, including prostate, breast, pancreatic, ovarian, and lung cancers. Therefore, AXL and ACK1 have been proposed as the attractive targets for cancer therapeutics and a number of small molecule inhibitors have been developed.
The purpose of this study is to develop the potent compounds as kinase inhibitors against AXL and ACK1. Many kinase inhibitors utilize the pyrimidine scaffold as a hinge anchor with various substitutions at 2- and 4-positions. In this work, a novel series of aminopyrimidine derivatives, based on the structural features of TP-0903 and TAE-684 as AXL and ACK1 inhibitors, were designed and synthesized. The in vitro enzyme inhibitory activities against AXL and ACK1 for the synthesized compounds were tested.
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| E-mail |
jurisuh21@gmail.com |
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123rd General Meeting of the KCS