The best result was obtained for 5c with an IC 50 of 5 μM for both enzymes. The synthesized dual-acting agents exhibited promising inhibitory activities towards HDAC1 and CK2. Our bifunctional compounds combine two complementary chemo-active prototypical scaffolds: a hydroxamate essential for the chelation of the zinc ion present in the active site of HDAC (Zinc Binding Group), and a 4,5,6,7-tetrabromobenzotriazole ( TBB) moiety introduced to interact with the ATP binding site in CK2 and to act simultaneously as the cap group in the interaction with HDAC1. We disclose herein a series of novel dual inhibitors to target histone deacetylase 1 (HDAC 1) and protein kinase CK2. Drug entities able to address multiple targets can be more effective than those directed to just one biological target.
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