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Open AccessArticle

Kinase Inhibitory Activities and Molecular Docking of a Novel Series of Anticancer Pyrazole Derivatives

1
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University (Girls), Cairo 11754, Egypt
2
Department of Therapeutical Chemistry, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Giza 12622, Egypt
3
Pharmaceutical Chemistry Department, Drug Exploration & Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
4
Organic Chemistry Department, Faculty of Science, Al-Azhar University, Cairo 11651, Egypt
5
Pharmacognosy Department, Drug Bioassay-Cell Culture Laboratory, National Research Center, Dokki, Giza 12622, Egypt
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(12), 3074; https://doi.org/10.3390/molecules23123074
Received: 4 November 2018 / Revised: 22 November 2018 / Accepted: 22 November 2018 / Published: 24 November 2018
A series of novel 1,3,4-triarylpyrazoles containing different heterocycles has been prepared, characterized and screened for their in vitro antiproliferative activity against HePG-2, MCF-7, PC-3, A-549 and HCT-116 cancer cell lines. The biological results revealed that compound 6 showed the highest anticancer activity so it was subjected to a kinase assay study where it reduced the activity of several protein kinases including AKT1, AKT2, BRAF V600E, EGFR, p38α and PDGFRβ at 100 μM using the radiometric or ADP-Glo assay method. Molecular docking simulation supported the initial kinase assay and suggested a common mode of interaction at the ATP-binding sites of these kinases, which demonstrates that compound 6 is a potential agent for cancer therapy deserving further research. View Full-Text
Keywords: triarylpyrazole derivatives; triazolo[1,5-a]pyridines; anticancer activity; EGFR; molecular docking triarylpyrazole derivatives; triazolo[1,5-a]pyridines; anticancer activity; EGFR; molecular docking
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Nossier, E.S.; Abd El-Karim, S.S.; Khalifa, N.M.; El-Sayed, A.S.; Hassan, E.S.I.; El-Hallouty, S.M. Kinase Inhibitory Activities and Molecular Docking of a Novel Series of Anticancer Pyrazole Derivatives. Molecules 2018, 23, 3074.

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