Synthesis of Diazonamides

描述：(申请人提供)本研究的长期目标 程序针对重氮胺的合成，以及 也可能表现出细胞毒活性的中间体。这些重氮胺是 具有细胞毒性的海洋天然产物具有前所未有的结构 其他化合物。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 细胞数(IC50<15 ng/m L)。合成研究的一部分将涉及 生成应添加到pi缺陷的持久性自由基中间体 杂环和形成关键的中心受阻键存在于 重氮酰胺类药物。

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.