TOTAL SYNTHESIS OF THE FARNESY TRANSFERASE INHIBITOR

法尼西转移酶抑制剂的全合成

• 批准号: 6386525
• 负责人: JAMES L LEIGHTON
• 金额: $ 17.55万
• 依托单位: COLUMBIA UNIV NEW YORK MORNINGSIDE
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-09-01 至 2003-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6386525
• 关键词: Diels Alder reaction; alkyltransferase; antineoplastics; bicyclic compound; biological products; drug design /synthesis /production; enzyme inhibitors; molecular rearrangement

DESCRIPTION: (Applicant's Abstract) This project concerns the development of an efficient synthesis of CP-263,114, a structurally novel protein farnesyl transferase inhibitor of interest for its potential as an anti-cancer agent. The research has been designed not only to provide access to the natural product itself, but also to a series of analogs which could prove valuable for insight into the nature of the interaction between CP-263, 114 and its biological target. Chemically, the approach to be taken involves both the development of new chemistry and the use of powerful reactions in new contexts to achieve the synthesis in an efficient manner. This will lead to delineation of the chemistry of the unusual ring system of CP-263,114, and to understanding of the principles governing the reaction chemistry that we bring to bear on the problem. Such understanding could ultimately find application to other synthetic endeavors.

描述：（申请人摘要）该项目涉及开发 高效合成结构新颖的蛋白质法尼基 CP-263,114 转移酶抑制剂因其作为抗癌剂的潜力而受到关注。 该研究的目的不仅是为了提供接触自然的机会 产品本身，以及一系列可能被证明有价值的类似物 深入了解 CP-263、114 及其之间相互作用的本质 生物靶标。 从化学角度来说，所采取的方法涉及开发新的 化学以及在新环境中使用强大的反应来实现 以有效的方式进行合成。这将导致划定 CP-263,114 的不寻常环系统的化学，并了解 控制我们施加的反应化学的原则 问题。这种理解最终可以应用于其他领域 综合努力。