Acton E M, Tong G L, Mosher C W, Wolgemuth R L
J Med Chem. 1984 May;27(5):638-45. doi: 10.1021/jm00371a014.
3'-Deamino-3'-(3-cyano-4-morpholinyl)doxorubicin is a new analogue that is 100 to 1000 times more potent than doxorubicin against tumors in cell culture or in mice, that is active by intraperitoneal, intravenous, or oral dosing, and that does not produce chronic myocardial lesions in mice. This analogue was encountered in studies on the reductive alkylation of doxorubicin and daunorubicin with 2,2' - oxybis [acetaldehyde], which constructs a morpholino ring incorporating the amino N. The morpholinyl nitrile byproducts are separated by virtue of their nonbasicity from the expected morpholino derivatives. The 13-dihydro and 5-imino derivatives are also described in this important new class of anthracyclines.
3'-脱氨基-3'-(3-氰基-4-吗啉基)阿霉素是一种新的类似物，在细胞培养或小鼠体内对肿瘤的效力比阿霉素强100至1000倍，可通过腹腔注射、静脉注射或口服给药，且在小鼠体内不会产生慢性心肌损伤。这种类似物是在对阿霉素和柔红霉素与2,2'-氧双[乙醛]进行还原烷基化的研究中发现的，该反应构建了一个包含氨基N的吗啉环。吗啉基腈副产物因其非碱性而与预期的吗啉基衍生物分离。本文还描述了这一重要的新型蒽环类化合物中的13-二氢和5-亚氨基衍生物。
