Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 65, Issue -, Pages 205-222Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.04.051
Keywords
Pyrrolo[1,2-a]quinoxaline; Protein kinase CK2; Antiproliferative activity; Synthesis
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Funding
- Ligue Nationale contre le Cancer (Comite d'Aquitaine-Charentes, Bordeaux, France)
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Herein we describe the synthesis and properties of substituted phenylaminopyrrolo[1,2-a]quinoxalinecarboxylic acid derivatives as a novel class of potent inhibitors of the human protein kinase CK2. A set of 15 compounds was designed and synthesized using convenient and straightforward synthesis protocols. The compounds were tested for inhibition of human protein kinase CK2, which is a potential drug target for many diseases including inflammatory disorders and cancer. New inhibitors with IC50 in the micro- and sub-micromolar range were identified. The most promising compound, the 4-[(3-chlorophenyl)amino]pyrrolo[1,2-a]quinoxaline-3-carboxylic acid 1c inhibited human CK2 with an IC50 of 49 nM. Our findings indicate that pyrrolo[1,2-a]quinoxalines are a promising starting scaffold for further development and optimization of human protein kinase CK2 inhibitors. (C) 2013 Elsevier Masson SAS. All rights reserved.
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