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제114회 대한화학회 학술발표회, 총회 및 기기전시회 Synthesis and evaluation of 5-(3-(pyrazin-2-yl)benzylidene)thiazolidine-2,4-dione derivatives as pan-Pim kinases inhibitors

등록일
2014년 8월 28일 15시 14분 28초
접수번호
1063
발표코드
MEDI.P-961 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 15일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
박종성, HONG VICTOR SUKBONG, 이진호*
계명대학교 화학과, Korea
Pim kinases are frequently overexpressed in leukemia, lymphoma and some solid tumors. Pim kinases are involved in many cellular phenomena such as transcription, translation, growth, survival and apoptosis resistance of cancer cell. Thus, Pim kinases are considered as a potential target for cancer therapy. A novel series of 5-benzylidenethiazolidine-2,4-diones were synthesized as Pim kinases inhibitors. The structure-activity relationships (SAR) studies were performed. Hydroxyl group at 2-position of the benzene ring in 5-benzylidenethiazolidine-2,4-dione was found to be important for inhibitory activity against Pim kinases. Introduction of a pyrazinyl group at 5-position of the benzene ring of 5-benzylidenethiazolidine-2,4-dione improved activity significantly. Potency of the synthesized compound were improved against Pim-1 and Pim-3 kinase up to the detection limit, IC50< 0.0005 uM. Compound 5i showed dose-dependent anti-proliferative activity with 0.8 uM EC50 value in MV4-11 leukemia cell line.

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