Indeno[1,2-b]indole Inhibitors of Human Protein Kinase CK2 and Their Impact on Different Tumor Cell Lines (A021) - Université Claude Bernard Lyon 1 Accéder directement au contenu
Communication Dans Un Congrès Année : 2017

Indeno[1,2-b]indole Inhibitors of Human Protein Kinase CK2 and Their Impact on Different Tumor Cell Lines (A021)

Résumé

Increased protein kinase CK2 activity is involved in many human diseases such as cancer(Guisiano, S., et al. Eur. J. Cancer 2011, 47, 792–801). In consequence CK2 is an emerging major target for drug design. Several indeno[1,2-b]-indole-9,10-dione derivatives containing N5 -isopropyl substitutions on the C-ring were synthesized and have been reported as potent ATP-competitive CK2 inhibitors (Alchab, F., et al. Pharmaceuticals 2015, 8, 279–302; Gozzi, J.G., et al. J. Med. Chem. 2015, 58, 265–277). Here we report on the evaluation of these inhibitors, containing different substituents in the Aand D-rings, for their effects on various tumor cell lines: breast cancer cells MCF-7, lung carcinoma cells A427 and epidermal cancer cell line A431. The most potent CK2 inhibitor contains an O-prenyl residue R1 and exhibits an IC50 value of 0.025 µM. Treatment of MCF-7 cells with 20 µM of that compound for 24 h results in a reduction of the total cell number by 90%. Most of the remaining cells exhibited apoptotic morphology and showed nearly none proliferating activity. In contrast treatment of A431 cells and A427 cells caused only a moderate decrease of cell proliferation by 30% for all tested compounds

Dates et versions

hal-01683452 , version 1 (30-01-2018)

Identifiants

Citer

Dagmar Aichele, Marc Le Borgne, Joachim Jose. Indeno[1,2-b]indole Inhibitors of Human Protein Kinase CK2 and Their Impact on Different Tumor Cell Lines (A021). Second International Electronic Conference on Medicinal Chemistry (ECMC-2), Nov 2016, Bâle, Switzerland. pp.15/A021, ⟨10.3390/ph10010020⟩. ⟨hal-01683452⟩
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