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학술발표회초록보기

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  • 03월 02일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제117회 대한화학회 학술발표회, 총회 및 기기전시회 Design, synthesis and evaluation of new pyrimidine derivatives for ALK/ROS1 inhibitors [동우화인켐㈜ 포스터상][동우화인켐㈜ 대학(원)생 선정 포스터상]

등록일
2016년 2월 17일 17시 14분 35초
접수번호
1003
발표코드
MEDI.P-450 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
4월 22일 (금요일) 13:00~14:30
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
문성웅, 윤창수1,*, 문봉진
서강대학교 화학과, Korea
1한국화학연구원 의약화학연구센터, Korea
Anaplastic lymphoma kinase (ALK) is one of the receptor tyrosine kinases (RTK) belonging to the insulin receptor family. Among various oncogenic fusion genes, ALK has obtained tremendous attention due to ALK-positive tumors found in various cancer types, such as anaplastic large cell lymphoma (ALCL), diffuse large B-cell lymphoma (DLBCL), and non-small-cell lung cancer (NSCLC). In 2011, crizotinib was first approved as an ALK inhibitor drug to treat ALK-positive NSCLC. Since the advent of crizotinib in clinics, crizotinib resistant mutants have been developed among patients treated with crizotinib within one to two years. Thus, discovery efforts for second-generation ALK inhibitors which could overcome crizotinib-resistant issues have been pursued comprehensively, resulting in development of a few cornerstone compounds, such as TAE684, LDK378 (ceritinib), and CH5424802 (alectinib). LDK378 is known to be 3 to 6-fold more active than crizotinib in cell cytotoxicity assays. In terms of crizotinib resistance issues, LDK378 turned out to be active against most of the resistant mutants, such as L1196M, G1269A, I1171T, and S1206Y, but ineffective against G1202R and F1174C. In this presentation, we will describe synthesis and biological evaluation of new pyrimidine derivatives to discover novel ALK/ROS1 inhibitors. Not only biological activity but pharmacological properties including brain blood barrier (BBB) penetration abilities will be discussed.

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