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.

项目描述：（申请人摘要）本项目涉及一个