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4-Phenethylthio-2-phenylpyrazolo[1,5-a][1,3,5]triazin-7(6H)-one
Molbank Pub Date : 2017-12-15 , DOI: 10.3390/m970
Sergey Smolnikov , Ekaterina Gorgopina , Vera Lezhnyova , Gwyneth Ong , Wai-Keung Chui , Anton Dolzhenko

Exploring the pharmacologically important pyrazolo[1,5-a][1,3,5]triazin-7(6H)-one scaffold for the construction of new bioactive compounds, we developed a synthesis of 4-phenethylthio-2-phenylpyrazolo[1,5-a][1,3,5]triazin-7(6H)-one (4) via S-alkylation of 2-phenyl-4-thioxopyrazolo[1,5-a][1,3,5]triazine-7(6H)-one (3), prepared by the double ring closure of pyrazole and triazine rings upon the treatment of 1-cyanoacetyl-4-benzoylthiosemicarbazide (2) with alkali. The antiproliferative activity of 4 against human lung cancer (A549) and human breast cancer (MDA-MB231) cell lines was investigated. Compound 4 was found to be more active against lung cancer cells than breast cancer cells.

中文翻译:

4-Phenethylthio-2-phenylpyrazolo [1,5-a] [1,3,5] triazin-7(6H)-one

探索具有重要药理作用的吡唑并[1,5-a] [1,3,5]三嗪-7(6H)-一个用于构建新的生物活性化合物的支架,我们开发了4-苯乙硫基-2-苯基吡唑并[1]的合成​​方法。 ,5-a] [1,3,5] triazin-7(6H)-一(4)通过2-苯基-4-硫代吡唑并[1,5-a] [1,3,5]三嗪的S-烷基化-7(6H)-一(3),通过用碱处理1-氰基乙酰基-4-苯甲酰基硫代氨基脲(2)进行吡唑和三嗪环的双环闭合而制得。研究了4对人肺癌(A549)和人乳腺癌(MDA-MB231)细胞系的抗增殖活性。发现化合物4比乳腺癌细胞对肺癌细胞更具活性。
更新日期:2017-12-15
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