We found a match
Your institution may have rights to this item. Sign in to continue.
- Title
Kinase Inhibitory Activities and Molecular Docking of a Novel Series of Anticancer Pyrazole Derivatives.
- Authors
Nossier, Eman S.; Abd El-Karim, Somaia S.; Khalifa, Nagy M.; El-Sayed, Ali S.; Hassan, Emad S. I.; El-Hallouty, Salwa M.
- Abstract
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.
- Subjects
PYRAZOLE derivatives; ANTINEOPLASTIC agents; CANCER cell proliferation; MOLECULAR docking; PROTEIN kinases; CANCER treatment
- Publication
Molecules, 2018, Vol 23, Issue 12, p3074
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23123074