SYNTHESIS OF ENEDIYNE AGENTS

这项研究计划的目标是完成合成 Calicheamicinone，并将其改造成对映异构体。会的 是最短的合成至少十步。为了合成 异钙霉素，2，3-氮杂环丙烷类似物 (前体药物)在氮杂环被打开之前不能形成1，4-二基的 (重新安排)。动力米星核心结构和结构的进一步研究 将完成其合成工作。多环芳烃的合成 利用从我们的研究中学到的信息 关于新卡西诺抑素核心的工作将进行研究。新型合成材料 将制定方法来协助解决上述具体问题。 所有的研究目标都具有潜在的抗肿瘤活性，并将 百时美施贵宝筛选。 此方案中包含的信息受患者保护 德克萨斯大学奥斯汀分校的申请： 欲了解更多信息，请致电(512)471-3966联系菲利普·马格努斯博士。

The objectives of this research program are to complete the synthesis of calicheamicinone and adapt it into an enantiospecific synthesis. It will be the shortest synthesis by at least ten steps. To synthesize isocalicheamicinone, an 2,3-aziridine analogue of calicheamicinone (prodrug) that cannot form a 1, 4-diyl until the aziridine ring is opened (rearranged). Further studies on the dynemicin core structure and completion of its synthesis will be undertaken. Synthesis of the kedarcidin enediyne core structure using the information learned from our work on the neocarzinostatin core will be studies. New synthetic methodology will be developed to assist in the above specific problems. All of the research targets have potential antitumor activity, and will be screened by Bristol-Myers Squibb. The information contained in this proposal is protected by a patient application by The University of Texas at Austin: For additional information contact Dr. Philip Magnus at (512) 471-3966.