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Molecules 2018, 23(10), 2657;

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

Chemistry Department, Faculty of Science, Assiut University, 71516 Assiut, Egypt
LCC-CNRS Université de Toulouse, CNRS, UPS, 205 Route de Narbonne, 3107 Toulouse, France
Aix-Marseille Université, CNRS, Institut de Chimie Radicalaire ICR, UMR 7273, Laboratoire de Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 27 Boulevard Jean Moulin CS 30064, 13385 Marseille CEDEX 05, France
Author to whom correspondence should be addressed.
Received: 8 August 2018 / Revised: 30 August 2018 / Accepted: 3 September 2018 / Published: 16 October 2018
(This article belongs to the Section Bioorganic Chemistry)
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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. View Full-Text
Keywords: pyrazolo[3,4-b]pyrazines; o-aminonitrosopyrazole; anticancer; anti-inflammatory; anti-breast cancer pyrazolo[3,4-b]pyrazines; o-aminonitrosopyrazole; anticancer; anti-inflammatory; anti-breast cancer

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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El-Kashef, H.; El-Emary, T.; Verhaeghe, P.; Vanelle, P.; Samy, M. Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines. Molecules 2018, 23, 2657.

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