TOTAL SYNTHESIS OF ANTITUMOR TAXANES

抗肿瘤紫杉烷的全合成

• 批准号: 3182777
• 负责人: ROBERT A HOLTON
• 金额: $ 26.72万
• 依托单位: FLORIDA STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1985
• 资助国家: 美国
• 起止时间: 1985-06-01 至 1995-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3182777
• 关键词: analog; antimitotics; antineoplastics; chemical condensation; cyclic ketone; diterpenes; drug design /synthesis /production; esterification; paclitaxel; stereoisomer

The development of synthetic methodology leading to the total synthesis of taxol is proposed. Taxol is one of the most potent new antitumor drug prospects, and it is currently in Phase III Clinical Trials against ovarian cancer and Phase II Clinical Trials against breast cancer. Other Clinical Trials are planned. The supply of taxol is currently severely limited, and development of synthesis of the drug will potentially solve this problem. In addition, this work will also provide the knowledge to permit the synthesis of a large number of taxol mimics, some of which are very likely to have better antitumor activity than taxol itself. These studies will also lead to a better understanding of taxol's mechanism of action, which, in turn, will lead to the development of new, superior taxol related drugs.

合成方法学的发展导致全合成 的紫杉醇。 紫杉醇是目前最有效的新型抗肿瘤药物之一 药物前景，目前正在进行III期临床试验， 卵巢癌和乳腺癌的II期临床试验。 计划进行其他临床试验。 紫杉醇的供应目前 严重限制，药物合成的发展将 有可能解决这个问题。 此外，这项工作还将 提供了合成大量紫杉醇的知识 模拟物，其中一些很可能具有更好的抗肿瘤活性 而不是紫杉醇本身。 这些研究也将导致更好的 了解紫杉醇的作用机制，这反过来将导致 开发新的、上级紫杉醇相关药物。