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

Submission Date :
2 / 12 / 2008 , 11 : 13 : 07
Abstract Number :
Presenting Type:
Poster Presentation
Presenting Area :
Authors :
권정진, 전문국1, 이덕형, 공영대1
서강대학교 화학과,
1한국화학연구원 신약기반기술연구센터,
Assigned Code :
33P227포 Assigend Code Guideline
Presenting Time :
목 <발표Ⅱ>
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.