TOTAL SYNTHESIS OF THE FARNESY TRANSFERASE INHIBITOR

法尼西转移酶抑制剂的全合成

• 批准号: 6182020
• 负责人: JAMES L LEIGHTON
• 金额: $ 17.05万
• 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/6182020
• 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：(申请者摘要)这个项目涉及到一个 结构新颖的法尼基蛋白质CP-263,114的高效合成 转移酶抑制剂因其作为抗癌药物的潜力而备受关注。 这项研究的设计不仅是为了提供进入自然环境的途径 产品本身，以及一系列类似的产品，这些产品可能被证明对 洞察CP-263、114与其相互作用的本质 生物目标。 在化学方面，将采取的方法包括开发新的 化学和在新的环境中使用强大的反应来实现 以有效的方式进行合成。这将导致对 CP-263,114的异常环系的化学和对 我们将反应化学的原理应用于 有问题。这样的理解最终可能适用于其他 综合努力。