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核苷酸生物合成的潜在抑制剂。1. 亚硝基脲核苷。2.

Potential inhibitors of nucleotide biosynthesis. 1. Nitrosoureidonucleosides. 2.

作者信息

Montgomery J A, Thomas H J, Brockman R W, Wheeler G P

出版信息

J Med Chem. 1981 Feb;24(2):184-9. doi: 10.1021/jm00134a011.

Abstract

Several nitrosoureidonucleosides (9a, 9b, 11a, 11b, 18 and 20) designed as inhibitors of enzymes that metabolize purine and pyrimidine nucleotides have been prepared and their chemical and biological properties studied. The low level of biological activity observed may be due to the unexpected stability of these nitrosoureas compared to biologically active compounds such as N-methyl-N-nitrosourea (MNU), N,N'-bis(2-chloroethyl)-N'-nitrosourea (BCNU), and N,N'-dicyclohexyl-N-nitrosourea (DCyNU).

摘要

已制备了几种被设计为嘌呤和嘧啶核苷酸代谢酶抑制剂的亚硝基脲核苷(9a、9b、11a、11b、18和20),并对其化学和生物学性质进行了研究。观察到的低生物活性水平可能是由于与生物活性化合物如N-甲基-N-亚硝基脲(MNU)、N,N'-双(2-氯乙基)-N'-亚硝基脲(BCNU)和N,N'-二环己基-N-亚硝基脲(DCyNU)相比,这些亚硝基脲具有意想不到的稳定性。

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