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新型4-重氮吡唑衍生物的合成及其抗肿瘤活性

Synthesis and antineoplastic activity of new 4-diazopyrazole derivatives.

作者信息

Daidone G, Maggio B, Raffa D, Schillaci D, Plescia S

机构信息

Dipartimento di Chimica e Tecnologie Farmaceutiche, Università di Palermo.

出版信息

Farmaco. 1997 Aug-Sep;52(8-9):557-9.

PMID:9507664
Abstract

Several new 4-diazopyrazole derivatives were synthesized by reaction of 1-(R-substituted)phenyl-3-methyl-5-benzamidopyrazoles with a sevenfold excess of nitrous acid in acetic media. The compounds were tested at 20 microM concentration for their antineoplastic activity in vitro against Raji (human Burkitt lymphoma), K562 (human chronic myelogenous leukemia) and U937 (human histiocytic lymphoma) cell lines. They showed a percent of growth inhibition in the range 23.4-100%.

摘要

通过使1-(R-取代的)苯基-3-甲基-5-苯甲酰胺基吡唑与在乙酸介质中过量七倍的亚硝酸反应,合成了几种新的4-重氮吡唑衍生物。在20微摩尔浓度下测试了这些化合物对Raji(人伯基特淋巴瘤)、K562(人慢性粒细胞白血病)和U937(人组织细胞淋巴瘤)细胞系的体外抗肿瘤活性。它们的生长抑制百分比在23.4%至100%的范围内。

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