Synthesis of Diazonamides

重氮酰胺的合成

• 批准号: 6723657
• 负责人: PHILIP D MAGNUS
• 金额: $ 24.51万
• 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 2005-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6723657
• 关键词: aldehydes; alkaloids; alkylation; amides; animal extract; antineoplastics; biotherapeutic agent; chemical synthesis; cytotoxicity; drug design /synthesis /production; heterocyclic compounds; indoles; ionization; marine toxins; neoplasm /cancer pharmacology; oxazoles; stereochemistry; stereoisomer

DESCRIPTION: (provided by applicant) 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 less than 15 ng/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.

描述：（由申请人提供）本研究的长期目标 程序针对重氮酰胺的合成，并且 也可能表现出细胞毒活性的中间体。重氮酰胺类药物是 具有前所未有的结构的细胞毒性海洋天然产物 其他化合物。据报道，diazonamide A 在体外具有强效 针对 HCT-116 人类结肠癌和 B-16 鼠黑色素瘤癌症的活性 细胞（IC50 小于 15 ng/mL）。部分综合研究将涉及 产生持久性自由基中间体，补充 pi 缺陷 杂环并形成存在于的关键中心受阻键 重氮酰胺类。