NEW SYNTHETIC REACTIONS FOR ACTIVE PRINCIPLES

公安部对这一项目抱有双重希望。首先，作为一种化学反应 实验室，他的团队提议开发新的能力 综合，包括战略和方法两个层面。 有机合成中的强度增强在 为生物检查组装复杂的分子。在 HL2588计划重点关注一组目标，本身就是， 从前景看好的临床前活动或 新的生物作用机制。因此，目标被选择 以期提供不同的合成，同时 在合成过程中提高新药先导的可能性 用于探索结构和机制问题的衬底。 大约三分之一的努力将被用于 碳水化合物合成。相当大的注意力被引导到 他计划的其他部分的合成侧重于各种化学物质 作为探索的一部分的问题，旨在全面合成一个 收集有趣且具有挑战性的自然产品目标 结构。在这些单独的天然产物衍生项目中 是磷脂酶抑制剂组胺(方案E)； 明胶(程序F)，CP 225,917，它是一种法尼基转移酶 抑制物(程序g)，wortmannin，一种细胞周期调节剂 (程序H)。他还试图追求完全合成 希司他丁，也是一种细胞周期调节剂(程序I)，螺旋前列腺素， 在G2/M期干预细胞周期进程的一种药物 阶段(方案J)，三环素，一种天然产品 乙酰胆碱酯酶活性(程序K)和二双内酯，一种蛋白质 磷酸酶抑制剂(项目L)。讨论了这项建议。 根据这些节目分类。

The PI's hopes for this project are twofold. First, as a chemistry laboratory, his group proposes to develop new capabilities in synthesis, both at the strategic and methodological levels. Enhancement of strength in organic synthesis finds ready application in assembling molecules of complexity for biological scrutiny. In the HL2588 Program the focus is on a group of targets which are, per se, of interest from the standpoint of promising pre-clinical activity or novel mechanism of biological action. Thus, the targets are selected with a view to providing differing syntheses, while at the same time raising the possibility of new drug leads in the course of synthesizing substrates for probing issues of structure and mechanism. Approximately a third of the effort will be directed toward carbohydrate synthesis. Considerable attention is to directed to the synthesis of the other part of his program focuses on diverse chemical issues as part of explorations directed to the total synthesis of a collection of interesting and challenging natural product goal structures. Among these individual natural product derived projects are the phospholipase inhibitor hispidospermidin (program E); gelsemine (program F), CP 225, 917, which is a farnesyl transferase inhibitor (program g), wortmannin, which is a cell cycle modulator (program H). He also seeks to pursue the total synthesis of himastatin, also a cell cycle modulator (program I), spirotryprostatin, an agent which intervenes in the cell cycle progression at the G2/M phase (program J), tricycloillicinone, a natural product which increases acetylcholinesterase activity (program K) and disydiolide, a protein phosphatase inhibitor (program L). The proposal was discussed according to these program classifications.