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新型2-、3-或4-取代吡啶并[2',3':3,4]吡唑并[1,5-a]嘧啶的体外合成及抗增殖活性

Synthesis and antiproliferative activity in vitro of new 2-, 3- or 4-substituted pyrido[2',3':3,4]pyrazolo[1, 5-a]pyrimidines.

作者信息

Poreba Krystyna, Wietrzyk Joanna, Opolski Adam

机构信息

Department of Technology of Drugs, Wrocław University of Medicine, Wrocław, Poland.

出版信息

Acta Pol Pharm. 2006 May-Jun;63(3):189-94.

Abstract

The synthesis of several new 2-, 3- or 4-substituted pyrido[2',3':3,4]pyrazolo[1,5-a]pyrimidines is described. The obtained compounds were tested for their antiproliferative activity in vitro. Two of them: 3-chloro-2-methylpyrido[2',3':3,4]pyrazolo[1,5-a] pyrimidin-4-one [X] and 2,3-cyclopentylpyrido [2',3':3,4] pyrazole[1,5-a]pyrimidin-4-one [XII] revealed weak cytotoxic activity against the cells of human bladder cancer cell lines: LoVo, MCF-7, MES-SA and HCTV29T. The structures of the products II - XII were established on the basis of elemental analysis and spectral data (IR, 1H NMR and MS).

摘要

描述了几种新的2-、3-或4-取代的吡啶并[2',3':3,4]吡唑并[1,5-a]嘧啶的合成。对所得到的化合物进行了体外抗增殖活性测试。其中两种:3-氯-2-甲基吡啶并[2',3':3,4]吡唑并[1,5-a]嘧啶-4-酮[X]和2,3-环戊基吡啶并[2',3':3,4]吡唑并[1,5-a]嘧啶-4-酮[XII]对人膀胱癌细胞系LoVo、MCF-7、MES-SA和HCTV29T的细胞显示出较弱的细胞毒性活性。产物II - XII的结构基于元素分析和光谱数据(红外光谱、1H核磁共振谱和质谱)确定。

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