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학술발표회초록보기

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  • 09월 08일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제116회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Novel 2,4-diarylaminopyrimidines as ALK inhibitors

등록일
2015년 9월 3일 16시 12분 37초
접수번호
1281
발표코드
MEDI.P-519 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 15일 (목요일) 11:00~12:30
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
Gangadhar Rao Mathi, 황종연1, 윤창수2, 정희정3, 하재두4, 조성윤4, 김형래4,*, 김필호5,*
과학기술연합대학원대학교(UST) 의약화학, Korea
1한국화학연구원 신약연구본부, Korea
2한국화학연구원 신약연구본부 의약화학연구센터, Korea
3한국화학연구원 의약화학연구센터, Korea
4한국화학연구원 난치성질환치료제연구센터, Korea
5한국화학연구원 난치성질환치료제연구그룹, Korea
Anaplastic lymphoma kinase (ALK) serves as a potent target for innovative combination therapies based on selective small-molecule inhibitors of its use as an oncoantigen for tumour vaccination. After the first ALK inhibitor, crizotinib (xalkori) developed by Pfizer, developed resistance, various efforts to overcome drug resistance issues have been actively pursued. In 2014, the second-generation ALK inhibitor ceritinib was approved by the US FDA for the treatment of patients with ALK-positive metastatic NSCLC, who were previously treated with, or resistant to crizotinib. In order to develop novel ALK inhibitors, a series of new 2,4-diaminopyrimidines were synthesized and investigated for their biological activities against ALK wild type as well as mutants to discover preclinical candidates. Compared with ceritinib, the biological activities obtained with our compounds were promising, providing an in-depth understanding and gave new insights in the further development to produce selective and potent ALK inhibitors. The design, synthesis, and SAR of these compounds will be described.

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