SYNTHESIS OF ENEDIYNE AGENTS

本研究计划的目标是完成以下内容的合成 加利车霉素酮并使其适应于对映体特异性合成。 它将 最短的合成，至少十步。 合成 异加利车霉素酮，加利车霉素酮2，3-氮丙啶类似物 在氮丙啶环打开之前不能形成1，4-二基的前药 （重新整理）。 动力霉素核心结构的进一步研究和 将着手完成综合报告。 合成 kedarcidin enediyne核心结构，使用从我们的 将对新制癌素核心进行研究。 新合成 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， 由Bristol-Myers Squibb筛选。 本建议书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与Philip Magnus博士联系。

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.