首页> 外国专利> OLIGOSACCHARIDES USED FOR INHIBITING THE MITOSIS OF ASTROCYTES AND TUMORAL CELLS OF THE NERVOUS SYSTEM, AND METHODS FOR OBTAINING THEM

OLIGOSACCHARIDES USED FOR INHIBITING THE MITOSIS OF ASTROCYTES AND TUMORAL CELLS OF THE NERVOUS SYSTEM, AND METHODS FOR OBTAINING THEM

机译:用于抑制星形胶质细胞和神经系统肿瘤细胞的寡糖的寡糖及其获得方法

摘要

The method for obtaining oligosaccharides starts with the allylation of position (3') of β-lactosides followed by the controlled benzylation which leads to perbenzylated and partially benzylated compounds. The latter are glycosylated in position 3, not benzylated, with a donor of α-L-fucopyranosyl to yield protected trisaccharides. These and perbenzylated β-lactosides are desallylated and, later, are glycosylated with a donator of 2-azido-2-desoxy-α-D-galactopyranosyl to yield protected tetrasaccharides and trisaccharides, respectively. The debenzylation of said products accompanied by the reduction of the azydo group and simultanious acetylation of the amino group produces intermediary products which, by O-desacetylation, leads respectively to the final tetrasaccharides and trisaccharides. The resulting oligosaccharides produce, in vitro, inhibition of the mitosis of astrocytes and tumoral cells of the nervous system and, for this reason, could be used for controlling the glial scar and for the treatment of tumours of the nervous system.
机译:获得寡糖的方法始于将β-乳糖苷的位置(3')烯丙基化,然后进行受控的苄基化,这导致过苄基化和部分苄基化的化合物。后者在3位被糖基化而不是被苄基化,并带有一个α-L-呋喃二糖基供体,得到被保护的三糖。将这些和过苄基化的β-乳糖苷脱盐,然后用2-叠氮基-2-脱氧-α-D-吡喃半乳糖基的供体糖基化,分别得到被保护的四糖和三糖。所述产物的脱苄基作用伴随着Azydo基团的还原和氨基的同时乙酰化产生中间产物,该中间产物通过O-去乙酰化分别产生最终的四糖和三糖。所得的寡糖在体外产生对神经系统星形胶质细胞和肿瘤细胞的有丝分裂的抑制作用,并且由于这个原因,可以用于控制神经胶质瘢痕和治疗神经系统肿瘤。

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