![]() ![]() All the compounds demonstrated low sub-micromolar inhibition of CK2α and antiproliferative activity against both breast and lung cancer cell lines (MCF-7, and A549, respectively), at low micromolar concentrations with N 2-regioisomers exhibiting higher activity than their corresponding N 1-isomers. New compounds were prepared via N-alkylation of TBBt followed by base-catalysed hydrolysis or hydrazinolysis. A new series of antiproliferative casein kinase 2α (CK2α) inhibitors were synthesized incorporating either a hydrophilic group (carboxylic or hydrazide) or a hydrophobic group (ester) at N 1 or N 2 of 4,5,6,7-tetrabromobenzotriazole (TBBt).
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