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

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. Som...

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Autores principales: El-Kashef, Hussein, El-Emary, Talaat, Verhaeghe, Pierre, Vanelle, Patrice, Samy, Maha
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222508/
https://www.ncbi.nlm.nih.gov/pubmed/30332801
http://dx.doi.org/10.3390/molecules23102657
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author El-Kashef, Hussein
El-Emary, Talaat
Verhaeghe, Pierre
Vanelle, Patrice
Samy, Maha
author_facet El-Kashef, Hussein
El-Emary, Talaat
Verhaeghe, Pierre
Vanelle, Patrice
Samy, Maha
author_sort El-Kashef, Hussein
collection PubMed
description 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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spelling pubmed-62225082018-11-13 Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines El-Kashef, Hussein El-Emary, Talaat Verhaeghe, Pierre Vanelle, Patrice Samy, Maha Molecules Article 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. MDPI 2018-10-16 /pmc/articles/PMC6222508/ /pubmed/30332801 http://dx.doi.org/10.3390/molecules23102657 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
El-Kashef, Hussein
El-Emary, Talaat
Verhaeghe, Pierre
Vanelle, Patrice
Samy, Maha
Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines
title Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines
title_full Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines
title_fullStr Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines
title_full_unstemmed Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines
title_short Anticancer and Anti-Inflammatory Activities of Some New Pyrazolo[3,4-b]pyrazines
title_sort anticancer and anti-inflammatory activities of some new pyrazolo[3,4-b]pyrazines
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222508/
https://www.ncbi.nlm.nih.gov/pubmed/30332801
http://dx.doi.org/10.3390/molecules23102657
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AT vanellepatrice anticancerandantiinflammatoryactivitiesofsomenewpyrazolo34bpyrazines
AT samymaha anticancerandantiinflammatoryactivitiesofsomenewpyrazolo34bpyrazines

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