Israel M, Airey J E, Murray R J, Gillard J W
J Med Chem. 1982 Jan;25(1):28-31. doi: 10.1021/jm00343a006.
The synthesis, cell growth-inhibitory activity, in vivo antileukemic activity, and extent of DNA binding of the alpha- and beta-anomeric 7-O-(3-amino-3,5-dideoxy-D-ribofuranosyl)daunomycinones and their trifluoroacetamides are described. These compounds are unique in that they are the first reported furanoside analogues of the antitumor antibiotics daunorubicin and adriamycin. Continuing analysis of structure-activity relationships amongst natural and semisynthetic anthracyclines fails to reveal a predictable relationship between in vivo antitumor activity and the in vitro properties of DNA complexation and cell growth inhibition.
描述了α-和β-异头物7-O-(3-氨基-3,5-二脱氧-D-核糖呋喃糖基)柔红霉素酮及其三氟乙酰胺的合成、细胞生长抑制活性、体内抗白血病活性以及DNA结合程度。这些化合物的独特之处在于它们是首次报道的抗肿瘤抗生素柔红霉素和阿霉素的呋喃糖苷类似物。对天然和半合成蒽环类药物之间构效关系的持续分析未能揭示体内抗肿瘤活性与DNA络合和细胞生长抑制的体外特性之间的可预测关系。
