Horton D, Priebe W
J Antibiot (Tokyo). 1981 Aug;34(8):1019-25. doi: 10.7164/antibiotics.34.1019.
The 14-azido-, 14-thiocyanato-, 14-acetoxy-, and 14-acetylthio- derivatives of 7-O-(3,4-di-O-acetyl-2,6-dideoxy-alpha-L-lyxo-hexopyranosyl)daunomycinone were synthesized by displacement reactions conducted on the corresponding 14-bromide. The in vivo antitumor activities of the products were compared with that of the 14-hydroxyl derivative in the murine P-388 lymphocytic leukemia assay. The 14-acetoxy derivative was highly active and of low toxicity; the other products showed negligible or low activities.
通过对相应的14-溴化物进行取代反应,合成了7-O-(3,4-二-O-乙酰基-2,6-二脱氧-α-L-吡喃来苏糖基)柔红霉素酮的14-叠氮基、14-硫氰酸根合、14-乙酰氧基和14-乙酰硫基衍生物。在小鼠P-388淋巴细胞白血病试验中,将产物的体内抗肿瘤活性与14-羟基衍生物的活性进行了比较。14-乙酰氧基衍生物具有高活性和低毒性;其他产物显示出可忽略不计的活性或低活性。