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| Type |
Poster Presentation |
| Area |
의약화학 |
| Room No. |
포스터발표장 |
| Time |
4월 20일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-458 |
| Subject |
Discovery of novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety as ALK inhibitor |
| Authors |
이동호, 장예린1, 이덕형, 윤창수1, 하재두2, 황종연1,*
서강대학교 화학과, Korea
1한국화학연구원 의약화학연구센터, Korea
2한국화학연구원 난치성질환치료제연구센터, Korea
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| Abstract |
A series of novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety were synthesized and evaluated for their anti-anaplastic lymphoma kinase (ALK) activities using enzymatic and cell-based assays. Amongst the compounds synthesized, compound 17b showed promising pharmacological results in in vitro, ex vivo, and pharmacokinetic studies. An in vivo efficacy study with compound 17b demonstrated highly potent inhibitory activity in H3122 tumor xenograft model mice. A series of kinase assays showed that compound 17b inhibited various kinases including FAK, ACK1, FGFR, RSK1, IGF-1R, among others, thus demonstrating its potential for synergistic anti-tumor activity and development as a multi-targeted non-small cell lung cancer (NSCLC) therapy. |
| E-mail |
leedh112577@gmail.com |
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119th General Meeting of the KCS