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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2+3 |
| Time |
10월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-294 |
| Subject |
Design, Synthesis, and Enzyme Inhibitory Activity of Novel Aminopyrimidinylisoindolines against FAK and ACK1 |
| Authors |
Min Jung Choi, Juseung Kim, 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 |
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that transduces signaling from a diverse group of stimuli to control a variety of cellular pathways and processes, including cell proliferation, migration, morphology, and cell survival. FAK is overexpressed in many tumors, including those derived from the head and neck, colon, breast, prostate, liver, and thyroid. 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, FAK and ACK1 have been proposed as potential targets in cancer therapy and small molecule inhibitors for use as potential cancer therapies have been developed.
The purpose of this study is to develop the potent compounds as dual kinase inhibitors against FAK and ACK1. Based on the structural features of PF-562,271 and ASP-3026 as FAK and ACK1 inhibitors, a series of aminopyrimidinylisoindoline derivatives were designed and synthesized. The enzymatic assay against FAK and ACK1 and cell-based assay against five cancer cell lines for the synthesized compounds were carried out. |
| E-mail |
minjung9416@hanmail.net |
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120th General Meeting of the KCS