N-substituted indole-2 and 3-carboxamide derivatives as inhibitors of human protein kinase CK2: In vitro assay and molecular modelling study
Acta Chimica Slovenica, cilt.60, sa.3, ss.628-635, 2013 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 60 Sayı: 3
- Basım Tarihi: 2013
- Dergi Adı: Acta Chimica Slovenica
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.628-635
- Anahtar Kelimeler: Casein Kinase-2, Docking, Indole derivatives, Inhibitors
- Ankara Üniversitesi Adresli: Evet
Özet
Protein kinase CK2 (Casein Kinase 2) is involved in cell growth; proliferation and suppression of apoptosis. Hence, it strongly promotes cell survival and can be considered an important target for human cancers. In the present study, a series of N-substituted indole-2- and 3-carboxamide derivatives were tested for inhibitions of human recombinant protein kinase CK2 to evaluate their anticancer properties. The inhibition test revealed that the most active compound 4 (1-benzyl-N-(2,4-dichlorobenzyl)-1H-indole-2-carboxamide) showed an IC50 value of 14.6 μM towards human protein kinase CK2. A molecular docking study of the compounds with CK2 was performed and revealed the binding mode of the most active compound 4, underlying its inhibitory activity.