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5-苄基尿嘧啶、5-苯基胞嘧啶和5-苯基嘧啶-2-酮核苷对小鼠白血病L1210细胞尿苷磷酸化酶的抑制效力。

Inhibitory potency of 5-benzyluracil, 5-phenylcytosine and 5-phenylpyrimidin-2-one nucleosides against uridine phosphorylase from mouse leukemic L1210 cells.

作者信息

Votruba I, Krecmerová M, Hrebabecký H, Holý A

机构信息

Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Praha, Czech Republic.

出版信息

Nucleosides Nucleotides. 1999 Nov-Dec;18(11-12):2551-64. doi: 10.1080/07328319908044626.

Abstract

The inhibitory activity of a series of novel sugar-modified nucleosides derived from 5-benzyluracil, 5-phenylcytosine and 5-phenylpyrimidin-2-one against uridine phosphorylase purified from mouse leukemic L-1210 cells was investigated. Significant activity was encountered with O2,2'-anhydro-5-benzylcytidine hydrochloride, 2',3'-dideoxy-5-benzyluridine, 2',3'-dideoxy-4-thiouridine and alpha- and beta-anomers of 5-benzyl-1-(2-deoxy-D-arabino-hexopyranosyl)uracil.

摘要

研究了一系列源自5-苄基尿嘧啶、5-苯基胞嘧啶和5-苯基嘧啶-2-酮的新型糖修饰核苷对从小鼠白血病L-1210细胞中纯化得到的尿苷磷酸化酶的抑制活性。发现O2,2'-脱水-5-苄基胞苷盐酸盐、2',3'-二脱氧-5-苄基尿苷、2',3'-二脱氧-4-硫尿苷以及5-苄基-1-(2-脱氧-D-阿拉伯己吡喃糖基)尿嘧啶的α和β异头物具有显著活性。

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