SYNTHESIS OF DIAZONAMIDES

二氮酰胺的合成

• 批准号: 6137476
• 负责人: PHILIP D MAGNUS
• 金额: $ 16.21万
• 依托单位: UNIVERSITY OF TEXAS AT AUSTIN
• 依托单位国家: 美国
• 财政年份: 1990
• 资助国家: 美国
• 起止时间: 1990-04-01 至 2001-12-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6137476
• 关键词: alkaloids; amides; animal extract; antineoplastic antibiotics; cytotoxicity; drug design /synthesis /production; marine toxins; stereochemistry

The long term objectives of this research program are directed towards the synthesis of the diazonamides, and intermediates that may also exhibit cytotoxic activity. The diazonamides are cytotoxic marine natural products that have unprecedented structures unlike any other compounds. It was reported that diazonamide A has potent in vitro activity against HCT-116 human colon carcinoma and B-16 murine melanoma cancer cells (IC50 is less than 15ng/mL). Part of the synthetic studies will involve the generation of persistent radical intermediates that should add to pi-deficient heterocycles and form the key central hindered bond present in the diazonamides.

这项研究计划的长期目标是 重氮胺及其中间体的合成 显示出细胞毒活性。重氮酰胺是一种海洋细胞毒性物质 天然产品具有前所未有的结构，与其他任何产品都不同 化合物。据报道，重氮酰胺A具有体外效力。 抗人结肠癌HCT-116和小鼠黑色素瘤B-16的活性 癌细胞(IC50<15 ng/m L)。综合研究的一部分 将涉及产生持久的自由基中间体， 应该加到pi不足的杂环上，形成关键的中心 重氮酰胺中存在受阻的键。