1. Academic Validation
  2. Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2

Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2

  • Eur J Med Chem. 2013 Jul:65:205-22. doi: 10.1016/j.ejmech.2013.04.051.
Jean Guillon 1 Marc Le Borgne Charlotte Rimbault Stéphane Moreau Solène Savrimoutou Noël Pinaud Sophie Baratin Mathieu Marchivie Séverine Roche Andre Bollacke Adali Pecci Lautaro Alvarez Vanessa Desplat Joachim Jose
Affiliations

Affiliation

  • 1 Université Bordeaux Segalen, Pharmacochimie, FRE 3396, F-33000 Bordeaux, France. jean.guillon@u-bordeaux2.fr
Abstract

Herein we describe the synthesis and properties of substituted phenylaminopyrrolo[1,2-a]quinoxaline-carboxylic 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.

Keywords

Antiproliferative activity; Protein kinase CK2; Pyrrolo[1,2-a]quinoxaline; Synthesis.

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