Poreba Krystyna, Opolski Adam, Wietrzyk Joanna
Department of Technology of Drugs, Wrocław University of Medicine, Poland.
Acta Pol Pharm. 2002 May-Jun;59(3):215-22.
The synthesis of several new 3-substituted aminopyrazolo[3,4-b]pyridines is described. The obtained compounds were tested for their antiproliferative activity in vitro. Two of them: 3-chloroacetylaminopyrazolo[3,4-b]pyridine [II] and 3-(2-bromopropionyl-amino)pyrazolo[3.4-b]pyridine [III] revealed cytotoxic activity against the cells of 5 human tumor cell lines applied. Their ID50 values were in the range of the international activity criterion for synthetic agents (4 microg/ml). The structures of the products II-XVII were established on the basis of elemental analysis and spectral data (IR, 1H NMR and MS).
本文描述了几种新型3-取代氨基吡唑并[3,4-b]吡啶的合成。对所得到的化合物进行了体外抗增殖活性测试。其中两种化合物:3-氯乙酰氨基吡唑并[3,4-b]吡啶[II]和3-(2-溴丙酰基-氨基)吡唑并[3.4-b]吡啶[III]对所应用的5种人类肿瘤细胞系的细胞显示出细胞毒性活性。它们的半数抑制浓度(ID50)值在合成药物国际活性标准(4微克/毫升)范围内。产物II-XVII的结构是根据元素分析和光谱数据(红外光谱、1H核磁共振光谱和质谱)确定的。