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蒽环类抗生素方面已发现了一些具有较大治疗价值的高效和特效抗肿瘤药,如柔红霉素、阿霉素、表阿霉素、nogalamycin等,已用于临床治疗。然而,伴随其活性的高细胞毒性限制了临床的广泛使用。近来发现的具有较高疗效与较低毒副作用的新衍生物给这类药物带来了新希望。大约20个nogalamycin类似物通过标准的肿瘤细胞试验,其中menogaril的抗瘤谱最广。带瘤动物的中位生命延长率为84~131%。与阿霉素不同,它在Ames试验(鼠伤寒沙门氏菌)中不显示诱变性,这一特点导致了对该新化合物的广泛研究。以nogalamycin为原料,经半合成可得
Anthracyclines have found some of the more effective and effective anti-tumor drugs of great therapeutic value, such as daunorubicin, doxorubicin, epirubicin, nogalamycin, etc., have been used in clinical treatment. However, the high cytotoxicity associated with its activity limits the widespread clinical use. Recently discovered new derivatives with higher efficacy and less toxic side effects have brought new hope to these drugs. Approximately 20 nogalamycin analogs passed standard tumor cell assays, with menogaril having the broadest anti-tumor spectrum. The median lifespan of tumor-bearing animals is 84-131%. Unlike doxorubicin, it does not show mutagenicity in the Ames test (Salmonella typhimurium), a feature that has led to extensive research into this new compound. Nogalamycin as raw material, the semi-synthetic available