Florent J C, Genot A, Monneret C
Département de Pharmacognosie associé au CNRS, Université René Descartes, Paris, France.
J Antibiot (Tokyo). 1989 Dec;42(12):1823-30. doi: 10.7164/antibiotics.42.1823.
New anthracyclines including 2-deoxy-L-fucose, 2-deoxy-L-rhamnose and 2,6-dideoxy-2-iodo-alpha-L-mannose as sugar moieties, respectively 8, 11 and 14, have been obtained by glycosidation of the 4-demethoxy-9-hydroxymethyl-9-deacetyl daunorubicinone (1) with appropriate sugars under Koenigs-Knorr conditions. They were found to display high cytotoxicity on L1210 leukemia, but also an outstanding antileukemic activity in mice in the case of 8 and 14.
分别以2-脱氧-L-岩藻糖、2-脱氧-L-鼠李糖和2,6-二脱氧-2-碘-α-L-甘露糖作为糖部分的新型蒽环类化合物8、11和14,是通过在柯尼希斯-克诺尔条件下,用适当的糖对4-去甲氧基-9-羟甲基-9-脱乙酰柔红霉素酮(1)进行糖苷化反应得到的。它们在L1210白血病细胞上显示出高细胞毒性,并且在小鼠实验中,化合物8和14还表现出显著的抗白血病活性。