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  • 02월 22일 16시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

Novel Solid-Phase Synthetic method for 7-amido-1,4-benzodiazepine-2,5-dione derivatives

등록일
2008년 2월 12일 11시 13분 07초
접수번호
0875
발표코드
33P227포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 <발표Ⅱ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
권정진, 전문국1, 이덕형, 공영대1
서강대학교 화학과,
1한국화학연구원 신약기반기술연구센터,
The 1,4-benzodiazepine-2,5-dione derivatives have attracted much attention for their interesting biological properties including the potential as a scaffold for RGD peptidomimetics, GPIIbIIIa-fibrinogen interaction antagonistic activity for antithrombotic agents, p53-HDM2interaction antagonistic activity, cytotoxic and antiproliferative activities, cell adhesion inhibitory activity, and HDAC inhibitory activity for anticancer agents, IgE synthesis inhibitory activity in human B-cells for treatment of allergic diseases, GHS receptor antagonistic activity treatment of obesity and related disorders, and endothelin receptor antagonistic activity. We establishished the novel efficient protocol for the construction of 1,4-benzodiazepine-2,5-dione skeleton utilizing the resin bound anthranilic acid derivatives. The reaction sequence, reductive alkylation/N-protected amino acid coupling/deprotection-cyclization, was unprecedented even in solution phase and in particular the intermediated resin 2 enable us to exploit the diverse amino-related sunctionalities at the 7 position of the scaffold.

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