2006
DOI: 10.1021/jm050048t
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Evaluation of 3-Carboxy-4(1H)-quinolones as Inhibitors of Human Protein Kinase CK2

Abstract: Due to the emerging role of protein kinase CK2 as a molecule that participates not only in the development of some cancers but also in viral infections and inflammatory failures, small organic inhibitors of CK2, besides application in scientific research, may have therapeutic significance. In this paper, we present a new class of CK2 inhibitors-3-carboxy-4(1H)-quinolones. This class of inhibitors has been selected via receptor-based virtual screening of the Otava compound library. It was revealed that the most… Show more

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Cited by 59 publications
(32 citation statements)
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“…The cyclization of the enamines 16 is realized by the action of heat in high-boiling solvents such as biphenyl [44], biphenyl ether [1, 26,32,34,36,37,41,42,[45][46][47], Dowtherm A [35,38,39,48,49], and mineral oil [1] or by using effective cyclization agents such as polyphosphoric acid or its esters [1, 2], the halogen derivatives of phosphorus [1], ZnCl 2 [1], conc. sulfuric acid in mixture with acetic anhydride [1], and Eaton's reagent (a mixture of phosphorus(V) oxide and methanesulfonic acid) [37,40].…”
Section: Type Dmentioning
confidence: 99%
See 1 more Smart Citation
“…The cyclization of the enamines 16 is realized by the action of heat in high-boiling solvents such as biphenyl [44], biphenyl ether [1, 26,32,34,36,37,41,42,[45][46][47], Dowtherm A [35,38,39,48,49], and mineral oil [1] or by using effective cyclization agents such as polyphosphoric acid or its esters [1, 2], the halogen derivatives of phosphorus [1], ZnCl 2 [1], conc. sulfuric acid in mixture with acetic anhydride [1], and Eaton's reagent (a mixture of phosphorus(V) oxide and methanesulfonic acid) [37,40].…”
Section: Type Dmentioning
confidence: 99%
“…In addition, active researches have been carried out on other types of biological activity in 4-quinolones. The following types of activity have been observed in a series of papers: Antiviral with respect to hepatitis B, C, and HIV viruses [3,4,24] and herpes viruses [3,37], antiallergic [3], antimalarial [68,109], antitubercular [36,39,110], immunomodulating [38], antihypoxic [25], antidiabetic [46]. 4-Quinolones have antithrombocytic [111] and positive cardiotonic activity [24].…”
Section: Biological Activity Of 4-quinolonesmentioning
confidence: 99%
“…Even if antimony is a well-known toxic agent, it is used in anti-parasite therapies 172 and this compound can be interesting if related to the role of CK2 in parasite proliferation. The carboxyl acid moiety is also present in the dihydroquinoline derivates 173 selected via receptor-based virtual screening of the Otava compound library. The most active molecule, compound 7 (5,6,8-trichloro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, K i 5 0.06 mM), has been tested on a total of 8 PKs and it showed to inhibit CK2 and DYRK1a.…”
Section: Carboxyl Acid Derivativesmentioning
confidence: 99%
“…Earlier, we found protein kinase CK2 inhibitors among the derivatives of 3-carboxy-4(1H)-quinolone 30 . Recently, we have identified hit compound among the derivatives of 3-carboxy quinolin-2-one-7-bromo-2-oxo-1,2-dihydroquinoline-3-carboxylic acid 93 (Figure 1) which decreased activity of CK2 on 22% at concentration of 33 mM 31,32 .…”
Section: Resultsmentioning
confidence: 97%