Chiral Pyrazolo[4,3-e][1,2,4]triazine Sulfonamides—Their Biological Activity, Lipophilicity, Protein Affinity, and Metabolic Transformations
2021
Referring to our previous laboratory results related to the tyrosinase and urease inhibition
by pyrazolo[4,3-e][1,2,4]triazine sulfonamides, we examined here in silico the mechanism of action
at the molecular level of the investigated pyrazolotriazine sulfonamides by the molecular docking
method. The studied compounds being evaluated for their cytotoxic effect against cancer cell lines
(MCF-7, K-562) and for recombinant Abl and CDK2/E kinase inhibitory potency turned out to be
inactive in these tests. The pyrazolotriazines were also investigated with respect to their lipophilicity
and plasma protein binding using HPLC chromatography in isocratic conditions. The observed small
affinity for plasma proteins could be advantageous in the potential in vivo studies. Moreover, the
compounds were sensitive to metabolic transformations with phase I enzymes, which led to the
hydroxylation and dealkylation products, whereas phase II transformations did not occur.
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