N-substituted indole-2 and 3-carboxamide derivatives as inhibitors of human protein kinase CK2: In vitro assay and molecular modelling study

Ölgen S., Gratz A., KILIÇ KURT Z., Jose J.

Acta Chimica Slovenica, cilt.60, sa.3, ss.628-635, 2013 (SCI-Expanded) identifier identifier

  • 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.