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Novel Anti-cancer Agents as T-Type Calcium Channels Blockers

등록일
2008년 8월 12일 07시 24분 54초
접수번호
0969
발표코드
35P310포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 <발표Ⅰ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
최윤정, 서한나, 김수진, 임혜원1, 주동준, 이재열
경희대학교 화학과, Korea
1한국과학기술연구원 의과학연구센터, Korea
Calcium plays a critical role as an intracellular signal, and controls many different cell processes, of which calcium appears to play an important role in cell growth. For example, it has also been shown that calcium signaling is required for cell cycle progression from G1/S phase through to mitosis. It has been demonstrated that depletion of intracellular calcium arrests the cell cycle in the G0/G1 and S interphases. Regulation of the changes in intracellular calcium has been proposed to be via a T-type calcium channel. Therefore, novel T-type calcium channel blocker shows the possibility as new anti-cancer agent. Based on this finding, we have recently provided the evidence for the relationship between the inhibition of calcium influx and anti-cancer activity by usingthe library of 3,4-dihydroquinazoline derivatives. As a result of further structure-activity relationship study of these compounds, it was found that KYS05090 shows the comparable potency to Doxorubicin against 5 human cancer cell lines as well as high channel blocking activity (IC50 = 41 nM) against T-type calcium channel (1G).

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