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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| Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_02235234_v65_n_p205_Guillon http://hdl.handle.net/20.500.12110/paper_02235234_v65_n_p205_Guillon |
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paper:paper_02235234_v65_n_p205_Guillon2023-06-08T15:21:45Z Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a] quinoxaline derivatives as inhibitors of the human protein kinase CK2 Pecci, Adali 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. 2013 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_02235234_v65_n_p205_Guillon 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 Pecci, Adali 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. |
| author |
Pecci, Adali |
| author_facet |
Pecci, Adali |
| author_sort |
Pecci, Adali |
| 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 |
| publishDate |
2013 |
| url |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_02235234_v65_n_p205_Guillon http://hdl.handle.net/20.500.12110/paper_02235234_v65_n_p205_Guillon |
| work_keys_str_mv |
AT pecciadali synthesisandbiologicalevaluationofnovelsubstitutedpyrrolo12aquinoxalinederivativesasinhibitorsofthehumanproteinkinaseck2 |
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1768545689103499264 |