SYNTHESIS OF MACROCYCLIC ANTITUMOR ANTIBIOTICS

合成大环、双环和螺环单元的合成路线 存在于新型大环四酸抗肿瘤抗生素中， 将对其进行检测。苷元Kijanolide是最初的 此项目的目标。我们会特别注意 四酸亚结构和配基的大环环。这个 本文开发的合成方法将在合成中具有普遍的实用价值。 其他复杂的碳环物质，包括百里内酯和 河豚毒素-A单个单位及其组合代表了小说 具有潜在生物活性的结构在抗肿瘤和 抗生素区域。KijAnimicin显示出抗厌氧细菌的活性 并在小鼠身上起到抗疟疾的作用。Tetrocarin-A，一种与 抑制枯草杆菌RNA合成，抑制枯草杆菌生长 小鼠实验性肉瘤180和白血病P338肿瘤。

Synthetic routes to prototype macrocyclic, bicyclic, and spirocyclic units present in the novel macrocyclic tetronic acid antitumor antibiotic, kijanimicin, will be examined. The aglycone kijanolide is the initial target of this project. Particular attention will be accorded to the tetronic acid substructure and the macrocyclic ring of the aglycon. The synthetic methods developed here will have general utility in the synthesis of other complex carbocyclic substances, including chlorothricolide and tetrocarin-A. The individual units and their combinations represent novel structures with potential biological activity in the antitumor and antibiotic areas. Kijanimicin shows activity against anaerobic bacteria and acts as an antimalarial in mice. Tetrocarin-A, a close analog of kijanimicin, suppresses RNA synthesis in B. subtilis and inhibits growth of experimental sarcoma 180 and leukemia P338 tumors in mice.