Abstract
Identification of novel protein kinase CK2 inhibitors among indazole derivatives
Highlights
Casein kinase 2 (CK2) is a serine/threonine protein kinase usually consisting of two catalytic subunits (α) and/or (α’) and two regulatory (β) subunits
In order to provide enough hydrophobic interactions to keep binding in the pocket of ATPbinding site we have focused on a synthesis of indazole-carboxylic acids carrying the arylmoiety at the 3-rd position of the indazole ring
We are representing a method of synthesis of 3-phenyl-indazole-7-carboxylic acid that can be applied to the synthesis of any 3-aryl-substituted indazole-7-carboxy lic acid
Summary
Casein kinase 2 (CK2) is a serine/threonine protein kinase usually consisting of two catalytic subunits (α) and/or (α’) and two regulatory (β) subunits. This enzyme stands out among the most protein kinases by its high pleiotropicity. This ubiquity was considered as an obstacle to use CK2 in the drug development until discovering the fact that cancer cells are much more dependent on CK2 than normal cells [3] It has turned CK2 into an important player in overcoming drug resistance, albeit with some limitations [4].
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