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

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 pro...

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Autores principales:	Guillon, J., Le Borgne, M., Rimbault, C., Moreau, S., Savrimoutou, S., Pinaud, N., Baratin, S., Marchivie, M., Roche, S., Bollacke, A., Pecci, A., Alvarez, L., Desplat, V., Jose, J.
Formato:	JOUR
Materias:	Antiproliferative activity Protein kinase CK2 Pyrrolo[1,2-a]quinoxaline Synthesis carboxylic acid derivative casein kinase II quinoxaline derivative antiproliferative activity article cell strain K 562 controlled study drug screening drug synthesis human human cell IC 50 in vitro study leukemia cell molecular dynamics
Acceso en línea:	http://hdl.handle.net/20.500.12110/paper_02235234_v65_n_p205_Guillon
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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spelling	todo:paper_02235234_v65_n_p205_Guillon2023-10-03T15:11:16Z Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2 Guillon, J. Le Borgne, M. Rimbault, C. Moreau, S. Savrimoutou, S. Pinaud, N. Baratin, S. Marchivie, M. Roche, S. Bollacke, A. Pecci, A. Alvarez, L. Desplat, V. Jose, J. Antiproliferative activity Protein kinase CK2 Pyrrolo[1,2-a]quinoxaline Synthesis carboxylic acid derivative casein kinase II quinoxaline derivative antiproliferative activity article cell strain K 562 controlled study drug screening drug synthesis human human cell IC 50 in vitro study leukemia cell molecular dynamics 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 IC 50 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 IC 50 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. © 2013 Elsevier Masson SAS. All rights reserved. Fil:Pecci, A. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_02235234_v65_n_p205_Guillon
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic	Antiproliferative activity Protein kinase CK2 Pyrrolo[1,2-a]quinoxaline Synthesis carboxylic acid derivative casein kinase II quinoxaline derivative antiproliferative activity article cell strain K 562 controlled study drug screening drug synthesis human human cell IC 50 in vitro study leukemia cell molecular dynamics
spellingShingle	Antiproliferative activity Protein kinase CK2 Pyrrolo[1,2-a]quinoxaline Synthesis carboxylic acid derivative casein kinase II quinoxaline derivative antiproliferative activity article cell strain K 562 controlled study drug screening drug synthesis human human cell IC 50 in vitro study leukemia cell molecular dynamics Guillon, J. Le Borgne, M. Rimbault, C. Moreau, S. Savrimoutou, S. Pinaud, N. Baratin, S. Marchivie, M. Roche, S. Bollacke, A. Pecci, A. Alvarez, L. Desplat, V. Jose, J. Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
topic_facet	Antiproliferative activity Protein kinase CK2 Pyrrolo[1,2-a]quinoxaline Synthesis carboxylic acid derivative casein kinase II quinoxaline derivative antiproliferative activity article cell strain K 562 controlled study drug screening drug synthesis human human cell IC 50 in vitro study leukemia cell molecular dynamics
description	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 IC 50 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 IC 50 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. © 2013 Elsevier Masson SAS. All rights reserved.
format	JOUR
author	Guillon, J. Le Borgne, M. Rimbault, C. Moreau, S. Savrimoutou, S. Pinaud, N. Baratin, S. Marchivie, M. Roche, S. Bollacke, A. Pecci, A. Alvarez, L. Desplat, V. Jose, J.
author_facet	Guillon, J. Le Borgne, M. Rimbault, C. Moreau, S. Savrimoutou, S. Pinaud, N. Baratin, S. Marchivie, M. Roche, S. Bollacke, A. Pecci, A. Alvarez, L. Desplat, V. Jose, J.
author_sort	Guillon, J.
title	Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
title_short	Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
title_full	Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
title_fullStr	Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
title_full_unstemmed	Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2
title_sort	synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase ck2
url	http://hdl.handle.net/20.500.12110/paper_02235234_v65_n_p205_Guillon
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Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2

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