CAS: 5334-31-6; 3-Amino-1H-Pyrazole-4-Carboxamide

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📜3-氨基-4-氰基吡唑置于ammonium Hydroxide,硫酸体系中,用 水 作为反应溶剂,化学反应 5.0H,以90%的收率获得产物3-氨基-1H-吡唑-4-甲酰胺
参考文献:一些新型4,6-二取代吡唑并[3,4-D]嘧啶类化合物作为细胞周期蛋白依赖性激酶2(cdk2)抑制剂的合成,抗癌评估和分子对接研究
标题:一些新型4,6-二取代吡唑并[3,4-D]嘧啶类化合物作为细胞周期蛋白依赖性激酶2(cdk2)抑制剂的合成,抗癌评估和分子对接研究
摘要:一种新型系列的4,6-二取代的吡唑并[3,4的d]嘧啶(7-43)在在c-6位上c-4位和thiophenethyl或thiopentane部分轴承各种苯胺已设计并通过分子杂交的方法合成.对所有合成的化合物进行体外评估cdk2 / Cyclin E和abl激酶的抑制活性以及针对k-562(慢性粒细胞性白血病)和mcf-7(乳腺癌)的抗增殖活性.结构-活性关系(sar)研究表明,与c-6上的烷基(硫戊烷)和c-6上的双取代苯胺相比,C-6上具有噻吩乙基,C-4上具有单取代苯胺的化合物表现出更好的cdk2抑制活性.脚手架的c-4.特别地,在c-4具有2-氯,3-硝基和4-甲硫基苯胺基团的化合物显示出对cdk2的显着的酶抑制活性,其具有数位微摩尔ic 50值.将在硅片分子对接研究表明可能的结合方向和结合能与观测到的sar和实验结果一致.另外,一些合成的化合物以微摩尔范围的ic 50值显
DOI:10.1016/j.Bioorg.2018.02.030

专利信息

专利号:US-2022064167-A1
优先权日:2018-05-17
标 题 :Imidazo-pyrazole carboxamide derivatives as anticancer agents and the synthesis thereof
发明人：DEMJÉN ANDRÃ?S; Puskás László; KANIZSAI IVAN; SZEBENI GÃ?BOR; ANGYAL ANIKÓ; GYURIS Márió; Hackler László
权利人:AVIDIN KFT
摘要:The present invention relates to novel imidazo[1,2-b]pyrazole carboxamide and carbothioamide derivatives of general formula (V), and the advantageous derivatives and pharmaceutically acceptable salts thereof, the synthesis thereof, and medicinal and/or pharmaceutical composition comprising these compounds thereof and synthesis thereof, and for use as a medicament, for use in the treatment of different diseases, advantageously of cancer. The subject compounds are advantageously for use in the treatment of solid malignancies, advantageously breast, lung, melanoma, gliomas, and myeloproliferative and myelodysplastic neoplasms, acute myelogenous/myeloid leukemias and colon cancer by the differentiation and subsequent apoptosis of pre-matured myeloid leukemic cells or myeloid-derived suppressor cells and/or by direct effect on solid tumors.