ISOLATION AND STRUCTURE DETERMINATION OF CYANOBACTERIAL ANTITUMOR AGENTS

该实验室计划将为以下项目提供天然产品样品： NCNPDDG。 总共将有1,000种蓝绿藻（蓝藻） 每年用亲脂性和亲水性溶剂提取 系统 这些摘录将提交给韦恩州立大学， 分析. 表现出实体瘤和/或肿瘤选择性的提取物 活性将被分级分离，从而活性化合物可以被纯化 并鉴定 最高优先级将给予那些提取物， 对耐药实体瘤有活性。 我们预计， 0.5%的提取物将显示出值得追求的活性。 放大 然后将进行批量生产，以提供足够的材料用于体内 试验. 识别出的活动组件将启动模拟 合成程序以及通过两个Eli的库存搜索 Lilly和NCI进行类似物测试。 每单位约1个纯化化合物 预计2010年将开始药理学研究以及机制 行动研究。

This Laboratory Program will provide natural product samples for the NCNPDDG. A total of 1,000 blue-green algae (cyanobacteria) will be extracted each year with both a lipophilic and a hydrophilic solvent system. These extracts will be submitted to Wayne State University for analysis. Extracts which exhibit solid tumor and/or tumor selective activity will be fractionated so that the active compound can be purified and identified. Highest priority will be given to those extracts that are active against drug-resistant solid tumors. We expect that about 0.5% of the extracts will demonstrate activity worth pursuing. Scale-up batches will then be pursued to provide sufficient material for in vivo testing. The identified active component will initiate an analog synthesis program as well as a search through the inventories of both Eli Lilly and NCI for analogs to test. Approximately 1 purified compound per year is expected to begin pharmacological studies as well as mechanism of action studies.