1,1'-亚乙基-双(1-亚硝基脲)及相关化合物的化学稳定性、烷基化活性和亲脂性。

Chemical stability, alkylating activity, and lipophilicity of 1,1'-ethylene-bis(1-nitrosourea) and related compounds.

作者信息

Morimoto K, Yamaha T, Nakadate M, Suzuki I

出版信息

Gan. 1978 Feb;69(1):139-42.

Abstract

1,1'-Ethylene-bis(1-nitrosourea) (EBNU) posesses antitumor activity against leukemia L-1210. Chemical stability, alkylating activity, and lipophilicity of EBNU and related compounds were compared. EBNU was the most unstable among several bis-N-nitrosoureas and mono-N-nitrosoureas tested. The alkylating activity of EBNU was the same as that of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU), but higher than those of other bis- and mono-N-nitrosoureas except 1-methyl-1-nitrosourea. Lipophilicity of EBNU was extremely low compared with 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) and CCNU.

摘要

1,1'-亚乙基双(1-亚硝基脲)(EBNU)对白血病L-1210具有抗肿瘤活性。比较了EBNU及相关化合物的化学稳定性、烷基化活性和亲脂性。在测试的几种双N-亚硝基脲和单N-亚硝基脲中，EBNU是最不稳定的。EBNU的烷基化活性与1-(2-氯乙基)-3-环己基-1-亚硝基脲(CCNU)相同，但高于除1-甲基-1-亚硝基脲外的其他双N-亚硝基脲和单N-亚硝基脲。与1,3-双(2-氯乙基)-1-亚硝基脲(BCNU)和CCNU相比，EBNU的亲脂性极低。

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