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

제116회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Structural modifications of Nexavar central ring: Towards improved cellular anticancer potency and selective kinase profile

등록일
2015년 8월 27일 16시 12분 20초
접수번호
0979
발표코드
KCS.O-6 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 10시 : 00분
발표형식
구두발표
발표분야
Oral Presentation for Young International Chemists
저자 및
공동저자
ELDAMASY ASHRAF KAREEM AWAD MOHAMMED, 강순방1, 금교창2,*
과학기술연합대학원대학교(UST) 생물화학, Korea
1한국과학기술연구원(KIST) 뇌의약연구단, Korea
2한국과학기술연구원(KIST) 케모인포메틱스연구센터, Korea
New 2-quinolinyl and benzothiazole-2-yl amide and urea derivatives possessing the privileged pyridylamide moiety have been designed and synthesized as anticancer sorafenib congeners. Among the synthesized derivatives, 27 compounds were selected for evaluation of their antiproliferative activity over a panel of 60 cancer cell lines at a single dose concentration of 10 uM at National Cancer Institute (NCI, USA). Eight compounds, 9b?d, 9f, 13b, 14a, 14b, and 14d showed impressive growth inhibitory results and thus were further tested at 5-dose testing mode to determine their GI50 values. The data revealed that the ureidoquinolines 9b, 9d and ureidobenzothiazole 14b are the most active derivatives with significant efficacies and superior potencies surpassing sorafenib in the majority of the tested cancer cell lines, with submicromolar or one-digit GI50 values. Kinase screening of both 9d and 13b over a panel of oncogenic kinases at single dose of 10 uM revealed their selective inhibitory activities towards both BRAFV600E and C-RAF kinases, with IC50 values in nanomolar scale.

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