Journal: Scientific Reports

Article Title: Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation

doi: 10.1038/s41598-019-46287-5

Figure Lengend Snippet: Kinase Inhibitory Data of 1-(Substituted)phenyl-3-(4-(((5-phenyl-1 H -1,2,4-triazol-3-yl)methyl)thio)phenyl)urea Derivatives, 6a–i . Data are expressed as percentage of kinase inhibition at 10 μM test compound, obtained as mean of at least three determinations. Standard error of the mean (SEM) is ≤10%. Compound 6e displayed no inhibitory activity when tested against both AurA and AurB. Compound 6g displayed no inhibitory activity when tested against AurA. Compound 6h displayed no inhibitory activity when tested against AurB. The reference compound, DP01920, was not tested against both AurB and AurC.

Article Snippet: Compound 6a , merging the best inhibitory profile against the target c-Kit/AurB kinases, was tested on the human A2058 (American Type Culture Collection, Manassas, USA) and WM266-4 (European Collection of Authenticated Cell Cultures, Salisbury, UK) cell lines, chosen as representative of BRAF- mutated melanoma cell lines, to investigate its anti-proliferative efficacy.

Techniques: Inhibition, Activity Assay

Journal: Scientific Reports

Article Title: Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation

doi: 10.1038/s41598-019-46287-5

Figure Lengend Snippet: Binding pose of derivative 6a into the active site of AurB. The protein is represented as grey ribbons and light blue sticks, H-bonds are represented as yellow dashed lines.

Article Snippet: Compound 6a , merging the best inhibitory profile against the target c-Kit/AurB kinases, was tested on the human A2058 (American Type Culture Collection, Manassas, USA) and WM266-4 (European Collection of Authenticated Cell Cultures, Salisbury, UK) cell lines, chosen as representative of BRAF- mutated melanoma cell lines, to investigate its anti-proliferative efficacy.

Techniques: Binding Assay

Journal: Scientific Reports

Article Title: Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation

doi: 10.1038/s41598-019-46287-5

Figure Lengend Snippet: Inhibition of c-Kit and AurB phosphorylation by compound 6a in WM-266-4 and A-2058 cells after 72 h of treatment. The data are expressed as the ratio of phosphorylated c-Kit or AurB/total c-Kit or AurB. Columns and bars, mean values ± SD, respectively. *P < 0.05 vs. vehicle-treated controls.

Article Snippet: Compound 6a , merging the best inhibitory profile against the target c-Kit/AurB kinases, was tested on the human A2058 (American Type Culture Collection, Manassas, USA) and WM266-4 (European Collection of Authenticated Cell Cultures, Salisbury, UK) cell lines, chosen as representative of BRAF- mutated melanoma cell lines, to investigate its anti-proliferative efficacy.

Techniques: Inhibition, Phospho-proteomics