SYNTHESIS OF ANTITUMOR NATURAL PRODUCTS

抗肿瘤天然产物的合成

• 批准号: 6489019
• 负责人: YOSHITO KISHI
• 金额: $ 47.52万
• 依托单位: HARVARD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1978
• 资助国家: 美国
• 起止时间: 1978-03-17 至 2003-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6489019
• 关键词: analog; anthracyclines; antineoplastics; biological products; daunorubicin; drug design /synthesis /production; lactams; paclitaxel; tumor promoters

The major objective of this research is to make significant contributions to organic chemistry and medicine through studies directed towards the synthesis of natural products with antitumor activity or tumor-promoting activity, including halichondrins, C-indolactam V, cytoblastin, taxol/cephalomannine, mycalamides/onnamide, and daunomycin analogs. We believe that the power of organic chemistry, especially organic synthesis, is most effectively extended by challenging complex systems, and much of the progress of medicine certainly depends upon extension of the power of chemistry. More specifically, research efforts will be made first to develop general, flexible, and efficient syntheses of certain natural products and then to apply these to the synthesis of their analogs and derivatives, whose study will provide clues for developing better antitumor drugs or for understanding the tumor-promoting process. Among the five programs proposed, the halichondrin project is most advanced in our quest for an antitumor drug, and research plans are presented to identify a drug candidate for further clinical development.

这项研究的主要目标是做出重大贡献 通过针对有机化学和医学的研究 具有抗肿瘤或促肿瘤活性的天然产物的合成 活性，包括软海绵素、C-吲哚内酰胺 V、细胞增殖素、 紫杉醇/三尖杉宁碱、mycalamides/onnamide 和道诺霉素类似物。 我们 相信有机化学，特别是有机合成的力量， 通过挑战复杂的系统可以最有效地扩展，并且许多 医学的进步当然取决于力量的扩展 化学。 更具体地说，研究工作将首先 开发某些天然物质的通用、灵活和高效的合成方法 产品，然后将其应用于其类似物的合成 衍生品，其研究将为更好地开发提供线索 抗肿瘤药物或了解肿瘤促进过程。 之中 在提出的五个方案中，软海绵素项目在以下方面最为先进： 我们对抗肿瘤药物的探索以及研究计划已提交给 确定用于进一步临床开发的候选药物。