新型n -取代亚胺类抗癌药物的合成与研究

Dharam Paul Jindal , Vikas Bedi , Birinder Jit , Nalin Karkra , Sheetal Guleria , Ranju Bansal , Anja Palusczak , Rolf W. Hartmann
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引用次数: 15

摘要

以邻苯二酸酐、萘酸酐及其取代衍生物为原料,以2-肼-1-咪唑啉氢溴化物、各种对取代芳基胺、氨基酰硫胺和2,4-二硝基苯肼为原料,合成了一系列新的n -取代亚胺衍生物。化合物9、10、12、18、19、23、24和34-36经美国Bethesda国家癌症研究所筛选,具有抗肿瘤活性。为了研究n -取代对其治疗癌症的药理学特征的影响,一些新的氨基乙硫胺衍生物37-39也被制备出来。这些化合物(37-39)对人胎盘芳香化酶的抑制作用较弱。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and study of some new N-substituted imide derivatives as potential anticancer agents

A new series of N-substituted imide derivatives have been synthesized by treating phthalic anhydride, naphthalic anhydride and their substituted derivatives with 2-hydrazino-1-imidazoline hydrobromide, various para-substituted aryl amines, aminoglutethimide and 2,4-dinitrophenyl hydrazine. Compounds 9, 10, 12, 18, 19, 23, 24 and 34–36 have been selected and screened for antineoplastic activity by National Cancer Institute, Bethesda, USA. Some newer aminoglutethimide derivatives 37–39 have also been prepared in order to study the effect of N-substitution on its pharmacological profile for the treatment of carcinoma. These compounds (37–39) have exhibited weak inhibition of human placental aromatase as compared to aminoglutethimide.

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