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Pharmaceuticals 2015, 8(2), 279-302; doi:10.3390/ph8020279

Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2

1
EA 4446 Biomolécules Cancer et Chimiorésistances, SFR Santé Lyon-Est CNRS UMS3453 - INSERM US7, Faculté de Pharmacie - ISPB, Université Lyon 1, 8 avenue Rockefeller, F-69373, Lyon Cedex 8, France
2
Institut für Pharmazeutische und Medizinische Chemie, PharmaCampus, Westfälische Wilhelms-Universität Münster, Corrensstr. 48, 48149 Münster, Germany
3
Laboratoire Récepteurs à dépendance, UMR INSERM U1052/CNRS 5286, Centre de Recherche en Cancérologie de Lyon, Centre Léon Bérard, Cheney A, 28 rue Laënnec, F-69008, Lyon, France
4
Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstr. 1, 40225 Düsseldorf, Germany
5
ISM - CNRS UMR 5255, Université de Bordeaux, 351 cours de la Libération, F-33405 Talence cedex, France
6
ICMCB, UPR 9048, CNRS, Université de Bordeaux, 87, avenue du Docteur Schweitzer, F-33600 Pessac, France
7
Laboratoire ARNA, INSERM U869, UFR des Sciences Pharmaceutiques, Université de Bordeaux, 146 rue Léo Saignat, F-33076 Bordeaux cedex, France
8
Centre Commun de RMN, Université de Lyon, F-69003 Lyon, France
9
ESCPE Lyon, Université Lyon 1, 43 Bd du 11 Novembre 1918, F-69616 Villeurbanne Cedex, France
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 18 March 2015 / Accepted: 26 May 2015 / Published: 8 June 2015
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Abstract

Due to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design of ATP-competitive inhibitors of human CK2. In the present study, we prepared twenty-one indeno[1,2-b]indole derivatives, all of which were tested in vitro on human CK2. The indenoindolones 5a and 5b inhibited human CK2 with an IC50 of 0.17 and 0.61 µM, respectively. The indeno[1,2-b]indoloquinone 7a also showed inhibitory activity on CK2 at a submicromolar range (IC50 = 0.43 µM). Additionally, a large number of indenoindole derivatives was evaluated for their cytotoxic activities against the cell lines 3T3, WI-38, HEK293T and MEF. View Full-Text
Keywords: indeno[1,2-b]indoles; synthesis; protein kinase CK2; inhibitory activity; molecular modeling; cytotoxicity indeno[1,2-b]indoles; synthesis; protein kinase CK2; inhibitory activity; molecular modeling; cytotoxicity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Alchab, F.; Ettouati, L.; Bouaziz, Z.; Bollacke, A.; Delcros, J.-G.; Gertzen, C.G.; Gohlke, H.; Pinaud, N.; Marchivie, M.; Guillon, J.; Fenet, B.; Jose, J.; Borgne, M.L. Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2. Pharmaceuticals 2015, 8, 279-302.

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