SYNTHESIS OF AROMATIC ANTIBIOTICS AND ANTICANCER AGENTS

诺加洛尔、诺加霉素、6-脱氧-6-去甲基四环素的合成 类似物和橄榄石是这项建议的具体目标。 诺加罗一家 和诺加霉素是有效的抗癌剂。 奥利文是 橄榄霉素，其表现出抗生素和抗癌活性。 的 四环素类似物应表现出比四环素类似物更好的药代动力学特征。 许多四环素。 诺加罗和四环素合成的基础 是一个串联Claisen-Diels-桤木序列， 实验室 另外，蒽环类抗生素 骨架描述。 它应该是理想的建设， 11-脱氧蒽环类药物类似物。

The synthesis of nogarols, nogalamycin, 6-deoxy-6-demethyl-tetracycline analogs and olivin are the specific aims of this proposal. The nogarols and nogalamycin are potent anticancer agents. Olivin is part of olivomycin, which exhibits antibiotic and anticancer activity. The tetracycline analogs should exhibit better pharmacokinetic character than many tetracyclines. The basis for the nogarol and tetracycline syntheses is a tandem Claisen-Diels-Alder sequence which was developed in our laboratory. Additionally, a very direct route to the anthracycline skeleton is described. It should be ideal for the construction of many 11-deoxyanthracycline analogs.