TOTAL SYNTHESIS OF THE FARNESY TRANSFERASE INHIBITOR

法尼西转移酶抑制剂的全合成

• 批准号: 6526049
• 负责人: JAMES L LEIGHTON
• 金额: $ 18.07万
• 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/6526049
• 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.

项目描述：（申请人摘要）本项目涉及一种 CP-263，114的高效合成 转移酶抑制剂作为抗癌剂的潜力。 这项研究的目的不仅是为了让人们能够接触到自然环境， 产品本身，但也有一系列的类似物，可以证明有价值的， 深入了解CP-263，114及其 生物目标。 在化学上，所采取的方法既包括开发新的 化学和使用强大的反应在新的情况下，以实现 以高效的方式合成。这将导致划定的 CP-263，114的不寻常环系的化学，以及对 控制化学反应的原则，我们带来的影响， 问题.这种理解最终可以应用于其他 合成的努力。