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 ...
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La protéine kinase caséine kinase 2 (CK2) est une sérine/thréonine kinase hautement pléiotrope dont ...
Protein kinase CK2 is ubiquitous, essential and highly pleiotropic kinase whose abnormally high cons...
La protéine kinase CK2, au centre de la recherche biomédicale depuis plus de 50 ans, est une enzyme ...
The X-ray structure of the catalytic domain of the EphA3 tyrosine kinase in complex with a previousl...
Depuis la mise en évidence de l’existence des protéines kinases vers la fin des années 1950 cette fa...
Acute leukemia is a hematological malignancy with high incidence and recurrence rates, and is charac...
Leukemia is the most common blood cancer, and its development starts at diverse points, leading to d...
Human protein kinase CK2 has emerged as promising target for the treatment of neoplastic diseases. T...
Three different series of cis-restricted analogues of combretastatin A-4 (CA-4), corresponding to th...
Many polyphenolic compounds have been reported to inhibit protein kinases, with special reference to...
CK2 denotes a pleiotropic, constitutively active protein kinase whose abnormally high level in many ...
CK2 denotes a pleiotropic, constitutively active protein kinase whose abnormally high level in many ...
Our studies on the synthesis and biological evaluation of novel anticancer drugs consist of three re...
This PhD thesis work has been covered in the application of an integrated approach to get a better u...
SummaryProtein kinase CK2 is a multifunctional kinase of medical importance that is dysregulated in ...
La protéine kinase caséine kinase 2 (CK2) est une sérine/thréonine kinase hautement pléiotrope dont ...
Protein kinase CK2 is ubiquitous, essential and highly pleiotropic kinase whose abnormally high cons...
La protéine kinase CK2, au centre de la recherche biomédicale depuis plus de 50 ans, est une enzyme ...
The X-ray structure of the catalytic domain of the EphA3 tyrosine kinase in complex with a previousl...
Depuis la mise en évidence de l’existence des protéines kinases vers la fin des années 1950 cette fa...
Acute leukemia is a hematological malignancy with high incidence and recurrence rates, and is charac...
Leukemia is the most common blood cancer, and its development starts at diverse points, leading to d...
Human protein kinase CK2 has emerged as promising target for the treatment of neoplastic diseases. T...
Three different series of cis-restricted analogues of combretastatin A-4 (CA-4), corresponding to th...
Many polyphenolic compounds have been reported to inhibit protein kinases, with special reference to...
CK2 denotes a pleiotropic, constitutively active protein kinase whose abnormally high level in many ...
CK2 denotes a pleiotropic, constitutively active protein kinase whose abnormally high level in many ...
Our studies on the synthesis and biological evaluation of novel anticancer drugs consist of three re...
This PhD thesis work has been covered in the application of an integrated approach to get a better u...
SummaryProtein kinase CK2 is a multifunctional kinase of medical importance that is dysregulated in ...
La protéine kinase caséine kinase 2 (CK2) est une sérine/thréonine kinase hautement pléiotrope dont ...
Protein kinase CK2 is ubiquitous, essential and highly pleiotropic kinase whose abnormally high cons...
La protéine kinase CK2, au centre de la recherche biomédicale depuis plus de 50 ans, est une enzyme ...
