Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4- b]pyrazines

一些新型吡唑并[3,4-b]吡嗪的抗癌和抗炎活性

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作者:Hussein El-Kashef, Talaat El-Emary, Pierre Verhaeghe, Patrice Vanelle, Maha Samy

Abstract

New derivatives of pyrazolo[3,4-b]pyrazines and related heterocycles were synthesized using 5-amino-3-methyl-4-nitroso-1-phenyl-pyrazole (1) as a starting material. The 5-acetyl derivative 15 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 15 and 29 exhibited remarkable anti-inflammatory activity, where 15 showed the same activity as that of the reference drug indomethacin. On the other hand, compounds 25i, 25j showed very significant inhibitory activity (p < 0.001) against MCF-7 breast cancer cell line.

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