Tatsuta K
Gan To Kagaku Ryoho. 1984 Dec;11(12 Pt 2):2640-52.
Studies of anthracycline antibiotics which have been carried out for the purpose of finding compounds useful in the treatment of cancer are described. Synthetic development of derivatives and analogs which have stronger activities and lower characteristic toxicities than parent antitumor antibiotics such as daunomycin, adriamycin, etc., have been illustrated namely: (1) syntheses of 4'-O-derivatives such as 4'-O-tetrahydropyranyl-adriamycin; (2) syntheses of N-alkyl derivatives such as 3'-deamino-3'-morpholino-adriamycin; and (3) syntheses of 11-deoxy-adriamycin. Notably, 4'-O-tetrahydropyranyl-adriamycin having a (2" R)-configuration has been confirmed to have stronger activity and lower toxicity than adriamycin by Phase II study. New, naturally occurring anthracycline antibiotics (decilorubicin, arugomycin, ditrisarubicin, etc.) have also been reviewed.
描述了为寻找可用于治疗癌症的化合物而对蒽环类抗生素进行的研究。已举例说明了衍生物和类似物的合成进展,这些衍生物和类似物比柔红霉素、阿霉素等母体抗肿瘤抗生素具有更强的活性和更低的特征毒性,具体如下:(1)4'-O-衍生物的合成,如4'-O-四氢吡喃基-阿霉素;(2)N-烷基衍生物的合成,如3'-脱氨基-3'-吗啉代-阿霉素;以及(3)11-脱氧-阿霉素的合成。值得注意的是,通过II期研究证实,具有(2"R)-构型的4'-O-四氢吡喃基-阿霉素比阿霉素具有更强的活性和更低的毒性。还综述了新的天然存在的蒽环类抗生素(地西罗霉素、阿柔比星、双曲菌素等)。