一些新吡唑并[3,4-]吡嗪的抗癌和抗炎活性。

Chemistry Department, Faculty of Science, Assiut University, 71516 Assiut, Egypt.

LCC-CNRS Université de Toulouse, CNRS, UPS, 205 Route de Narbonne, 3107 Toulouse, France.

Molecules. 2018 Oct 16;23(10):2657. doi: 10.3390/molecules23102657.

New derivatives of pyrazolo[3,4-]pyrazines and related heterocycles were synthesized using 5-amino-3-methyl-4-nitroso-1-phenyl-pyrazole () as a starting material. The 5-acetyl derivative was shown to be a useful key intermediate for the synthesis of several derivatives of pyrazolopyrazines. Some of the prepared compounds were evaluated for their anti-inflammatory and anti-breast cancer MCF-7 cell line activities. SAR study showed that compounds and exhibited remarkable anti-inflammatory activity, where showed the same activity as that of the reference drug indomethacin. On the other hand, compounds , showed very significant inhibitory activity ( < 0.001) against MCF-7 breast cancer cell line.

使用 5-氨基-3-甲基-4-亚硝基-1-苯基-吡唑（）作为起始原料，合成了吡唑并[3,4-]吡嗪和相关杂环的新衍生物。显示 5-乙酰基衍生物是合成几种吡唑并吡嗪衍生物的有用关键中间体。对一些制备的化合物进行了抗炎和抗乳腺癌 MCF-7 细胞系活性的评价。SAR 研究表明，化合物和表现出显著的抗炎活性，其中表现出与参比药物吲哚美辛相同的活性。另一方面，化合物、表现出对 MCF-7 乳腺癌细胞系非常显著的抑制活性（<0.001）。