POTENTIAL ANTICANCER AGENTS .V. NEW AROMATIC NITROGEN NUSTARDS RELATED TO 3-[N,N-BIS(2-CHLOROETHYL)AMINO]-4-METHYLBENZOIC ACID

被引:16
作者
CAMBANIS, A
DOBRE, V
NICULESC.I
机构
[1] Oncological Institute, Bucharest
关键词
D O I
10.1021/jm00301a043
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of new esters and amides of 3-[N,N-bis(2-chloroethyl)amino]-4-methylbenzoic acid is described. New nitrogen mustards, derivatives of phosphoric and sulfonic aromatic acids, are also reported. A quantitative relation between hydrolysis rate of these N-mustards and basicity of precursor amines was established. Enhancement of the hydrolysis rate due to the steric effect of o-methyl groups was pointed out. Antitumor activity was tested against Jensen sarcoma, Walker 256 carcinosarcoma, and Guerin T8 carcinoma. © 1969, American Chemical Society. All rights reserved.
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页码:161 / &
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