Tolstikov V V, Kozlova N V, Iartseva I V, Preobrazhenskaia M N
Bioorg Khim. 1989 Feb;15(2):277-80.
Anthracycline antibiotics (daunorubicin, carminomycin and doxorubicin) N-acylated with antibiotic bruneomycin (streptonigrin) have been obtained from the parent compounds upon treatment with N, N'-dicyclohexylcarbodiimide and N-hydroxysuccinimide. These "chimeric" antibiotics are less active both in vitro and in vivo than the parent antibiotics. This demonstrates the stability of the intermolecular amide linkage in these compounds towards chemical and enzymatic hydrolysis as well as their inability to interact with corresponding receptors in contrast to less hindered derivatives of the parent antibiotics.
用N，N'-二环己基碳二亚胺和N-羟基琥珀酰亚胺处理蒽环类抗生素（柔红霉素、卡米诺霉素和阿霉素）后，得到了与抗生素布鲁诺霉素（链黑菌素）N-酰化的产物。这些“嵌合”抗生素在体外和体内的活性均低于母体抗生素。这表明这些化合物中分子间酰胺键对化学和酶促水解具有稳定性，并且与母体抗生素受阻较小的衍生物相比，它们无法与相应受体相互作用。
