Synthesis and antileukemic activity of ara-cytidylyl [5′→ 5′]-6-methylpurine riboside

…, IA Mikhailopulo, VP Reshchikov, NM Fertukova

Index: Kvasyuk, E. I.; Kulak, T. I.; Mikhailopulo, I. A.; Reshchikov, V. P.; Fertukova, N. M. Pharmaceutical Chemistry Journal, 1984 , vol. 18, # 3 p. 168 - 171 Khimiko-Farmatsevticheskii Zhurnal, 1984 , vol. 18, # 3 p. 304 - 307

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Abstract

The antileukemic activity of cytosine arabinoside (ara-C) is due to its conversion in the cell successively to the 5'-mono-, di-, and triphosphates [i]. This reaction competes with the catabolic deactivation of ara-C by deamination in the presence of cytidine deaminase [i]. Thus, the conversion of ara-C to its 5'-monophosphate (ara-CMP) is of crucial importance for the occurrence of physiological activity. This is the main reason for the interest of ...