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Keywords = triarylpyrazole derivatives

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18 pages, 3029 KiB  
Article
Kinase Inhibitory Activities and Molecular Docking of a Novel Series of Anticancer Pyrazole Derivatives
by Eman S. Nossier, Somaia S. Abd El-Karim, Nagy M. Khalifa, Ali S. El-Sayed, Emad S. I. Hassan and Salwa M. El-Hallouty
Molecules 2018, 23(12), 3074; https://doi.org/10.3390/molecules23123074 - 24 Nov 2018
Cited by 43 | Viewed by 4554
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 [...] Read more.
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. Full article
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20 pages, 2407 KiB  
Article
Synthesis of New Triarylpyrazole Derivatives Possessing Terminal Sulfonamide Moiety and Their Inhibitory Effects on PGE2 and Nitric Oxide Productions in Lipopolysaccharide-Induced RAW 264.7 Macrophages
by Mohammed S. Abdel-Maksoud, Mohammed I. El-Gamal, Mahmoud M. Gamal El-Din, Yunji Choi, Jungseung Choi, Ji-Sun Shin, Shin-Young Kang, Kyung Ho Yoo, Kyung-Tae Lee, Daejin Baek and Chang-Hyun Oh
Molecules 2018, 23(10), 2556; https://doi.org/10.3390/molecules23102556 - 7 Oct 2018
Cited by 12 | Viewed by 3208
Abstract
This article describes the design, synthesis, and in vitro anti-inflammatory screening of new triarylpyrazole derivatives. A total of 34 new compounds were synthesized containing a terminal arylsulfonamide moiety and a different linker between the sulfonamide and pyridine ring at position 4 of the [...] Read more.
This article describes the design, synthesis, and in vitro anti-inflammatory screening of new triarylpyrazole derivatives. A total of 34 new compounds were synthesized containing a terminal arylsulfonamide moiety and a different linker between the sulfonamide and pyridine ring at position 4 of the pyrazole ring. All the target compounds were tested for both cytotoxicity and nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Compounds 1b, 1d, 1g, 2a, and 2c showed the highest NO inhibition percentages and the lowest cytotoxic effect. The most potent derivatives were tested for their ability to inhibit prostaglandin E2 (PGE2) in LPS-induced RAW 264.7 macrophages. The IC50 for nitric oxide inhibition, PGE2 inhibition, and cell viability were determined. In addition, 1b, 1d, 1g, 2a, and 2c were tested for their inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) and Cyclooxygenase 2 (COX-2) protein expression as well as iNOS enzymatic activity. Full article
(This article belongs to the Section Medicinal Chemistry)
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