Journal
PHARMACEUTICALS
Volume 8, Issue 2, Pages 279-302Publisher
MDPI
DOI: 10.3390/ph8020279
Keywords
indeno[1,2-b]indoles; synthesis; protein kinase CK2; inhibitory activity; molecular modeling; cytotoxicity
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Funding
- Bonus Qualite Recherche (BQR) of the University Claude Bernard Lyon 1
- Cluster 5 Chimie Durable et Chimie pour la Sante of the Region Rhone-Alpes
- ARC 1 Sante of the Region Rhone-Alpes
- Institut des Sciences Pharmaceutiques et Biologiques (ISPB)
- Canceropole Lyon Auvergne Rhone-Alpes (CLARA)
- Universite France Allemagne (UFA) of ChemBioInteract network
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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 mu M, respectively. The indeno[1,2-b]indoloquinone 7a also showed inhibitory activity on CK2 at a submicromolar range (IC50 = 0.43 mu M). Additionally, a large number of indenoindole derivatives was evaluated for their cytotoxic activities against the cell lines 3T3, WI-38, HEK293T and MEF.
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