DESIGN AND SYNTHESIS OF SELECTIVE KINASE INHIBITORS
选择性激酶抑制剂的设计与合成
基本信息
- 批准号:2883041
- 负责人:
- 金额:$ 22.14万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:1997
- 资助国家:美国
- 起止时间:1997-03-01 至 2000-02-29
- 项目状态:已结题
- 来源:
- 关键词:
项目摘要
DESCRIPTION: The PI reports that the disruption of cellular signal
transduction via protein kinase (PK) malfunction has been related to the
onset of several disease states, including: rheumatoid arthritis, systemic
lupus erythematosis, diabetes mellitus, and Alzheimer's disease. He notes
that while PK inhibition is a logical target for chemotherapeutic
intervention, the structural homology among the many PK isozymes has impeded
the development of specific and hence therapeutically useful inhibitors. It
is indicated that some specificity has been achieved in the area of
indolocarbazoles and hence the archetypal naturally occurring congeners
staurosporine (1) and K252a (2) have been the focus of considerable
research. The PI states that this proposal describes: (A) preliminary
studies in which a concise synthesis of 2 has been achieved (eleven
synthetic operations, longest linear sequence of seven steps); and (B) the
application of this chemistry to the synthesis of 1 and analogs of 2 (i.e.,
3). It is reported that the latter analogs are targeted for use as probes
in a Chinese Hamster Ovary Cell assay developed at Yale and the capping
agent in a combinatorial peptide library that can be utilized to screen a
wide range of analogs for PK isozyme specificity. It is noted that finally,
efforts toward K252a have resulted in the development of novel carbenoid
reactions for which further research is proposed.
描述:PI报告了蜂窝信号的中断
项目成果
期刊论文数量(1)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
Rhodium carbenoid-initiated Claisen rearrangement: scope and mechanistic observations.
- DOI:10.1021/ol990697x
- 发表时间:1999-07
- 期刊:
- 影响因子:5.2
- 作者:J. Wood;G. Moniz
- 通讯作者:J. Wood;G. Moniz
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JOHN L WOOD其他文献
JOHN L WOOD的其他文献
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{{ truncateString('JOHN L WOOD', 18)}}的其他基金
Method and Strategy Development for the Synthesis of Physiologically Important Natural Products
合成具有生理重要性的天然产物的方法和策略开发
- 批准号:
10389539 - 财政年份:2021
- 资助金额:
$ 22.14万 - 项目类别:
Method and Strategy Development for the Synthesis of Physiologically Important Natural Products
合成具有生理重要性的天然产物的方法和策略开发
- 批准号:
10132361 - 财政年份:2020
- 资助金额:
$ 22.14万 - 项目类别:
Method and Strategy Development for the Synthesis of Physiologically Important Natural Products
合成具有生理重要性的天然产物的方法和策略开发
- 批准号:
10371896 - 财政年份:2020
- 资助金额:
$ 22.14万 - 项目类别:
Method and Strategy Development for the Synthesis of Physiologically Important Natural Products
合成具有生理重要性的天然产物的方法和策略开发
- 批准号:
10580775 - 财政年份:2020
- 资助金额:
$ 22.14万 - 项目类别:
Studies in the Synthesis of Physiologically Important
生理重要物质的合成研究
- 批准号:
7362069 - 财政年份:2007
- 资助金额:
$ 22.14万 - 项目类别:
Studies in the Synthesis of Physiologically Important
生理重要物质的合成研究
- 批准号:
6547101 - 财政年份:2002
- 资助金额:
$ 22.14万 - 项目类别:
Studies in the Synthesis of Physiologically Important
生理重要物质的合成研究
- 批准号:
7069986 - 财政年份:2002
- 资助金额:
$ 22.14万 - 项目类别:
Studies in the Synthesis of Physiologically Important
生理重要物质的合成研究
- 批准号:
6611357 - 财政年份:2002
- 资助金额:
$ 22.14万 - 项目类别:
Studies in the Synthesis of Physiologically Important
生理重要物质的合成研究
- 批准号:
6755957 - 财政年份:2002
- 资助金额:
$ 22.14万 - 项目类别:
Studies in the Synthesis of Physiologically Important
生理重要物质的合成研究
- 批准号:
6908180 - 财政年份:2002
- 资助金额:
$ 22.14万 - 项目类别:
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