|
|
| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2+3 |
| Time |
10월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-310 |
| Subject |
Design and synthesis of indazole derivatives as DYRK1B inhibitors |
| Authors |
Yeon Ji Park, Hyuk Lee1, Jaesook Yun*, Sung-Youn Chang1,*
Department of Chemistry, Sungkyunkwan University, Korea
1Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Korea
|
| Abstract |
Dual-specificity tyrosine phosphorylation-regulated kinase 1B (DYRK1B) is over-expressed in several different tumor types such as colon, ovarian, and pancreatic cancer. Recent studies have demonstrated inhibition of DYRK1B could be an attractive target for cancer therapy. In this study, we designed and synthesized indazole derivatives as novel DYRK1B inhibitor that ultimately can be developed as an anticancer drug. These derivatives exhibited potent inhibitory activity toward DYRK1B in an in vitro assay. Structure modification of indazole derivatives revealed structure-activity relationships for DYRK1B inhibition and enabled to design very potent DYRK1B inhibitors. We will measure the cytotoxicity by the CCK assay, the physical properties, and pharmacokinetic. |
| E-mail |
pkj461@hanmail.net |
|
120th General Meeting of the KCS