SYNTHESIS OF MACROCYCLIC ANTITUMOR ANIBIOTICS

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。这里开发的合成方法将具有 在合成其他复杂碳环物质中的一般用途。 各个单元及其组合代表了具有 在抗肿瘤和抗生素领域具有潜在的生物活性。 KijAnimicin显示出抗厌氧细菌的活性，并作为一种 小鼠的抗疟药。Tetrocarin-A，一种与KijAnimicin相近的类似物， 抑制枯草杆菌中RNA的合成并抑制实验性肺炎的生长 小鼠肉瘤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. The synthetic methods developed here will have general utility in the synthesis of other complex carbocyclic substances. 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.