SYNTHESIS AND CHARACTERIZATION OF STEROID-LINKED N-(2-CHLOROETHYL)NITROSOUREAS
SYNTHESIS AND CHARACTERIZATION OF STEROID-LINKED N-(2-CHLOROETHYL)NITROSOUREAS
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DOI：
10.1002/ardp.19893221206
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发表时间：
1989-12-01
影响因子：
5.1
通讯作者：
ZELEZNY, O
中科院分区：
文献类型：
--
作者：
EISENBRAND, G;FISCHER, J;ZELEZNY, O
Syntheses of steroid-linked N-[N''-(2-chloroethyl)-N''-nitrosocarbamoyl]-(CNC-)amino acid esters and -amides with potential antineoplastic activity are described. The esters are prepared by reaction by reaction of CNC-amino acids with steroids using N,N''-carbonyldiiimidazole and N,N''-dicylclohexylcarbodiimide. The corresponding amides are prepared by reaction of 1-(CNC-amino acyloxy)-pyrrerolidine-2,5-diones with 17.beta.-amino-3-hydroxy-1,3,5(10)-estratriene or 17.beta.-O-[4-(6-aminohexylamino)-1,4-dioxy-butyl]-estradiol. Estradiol-17.beta.-hemisuccinate is esterified with N-(2-hydroxyethyl)-N''-2(chloro-ethyl)-N''-nitrosourea (HECNU). Spectroscopic characteristics and relative binding affinities to steroid receptors are given.
