Synthesis and evaluation of new isatin-aminorhodanine hybrids as PIM1 and CLK1 kinase inhibitors

Creative Commons License

Khaldoun K., Safer A., Boukabcha N., DEGE N., Ruchaud S., Souab M., ...Daha Fazla

JOURNAL OF MOLECULAR STRUCTURE, cilt.1192, ss.82-90, 2019 (SCI-Expanded, Scopus)

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 1192
  • Basım Tarihi: 2019
  • Doi Numarası: 10.1016/j.molstruc.2019.04.122
  • Dergi Adı: JOURNAL OF MOLECULAR STRUCTURE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.82-90
  • Anahtar Kelimeler: Isatin-aminorhodanine, Microwave activation, Knoevenagel condensation, Kinase, RHODANINE DERIVATIVES, SCAFFOLD, SAR
  • Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
  • Ondokuz Mayıs Üniversitesi Adresli: Evet

Özet

A series of new hybrid isatin-aminorhodanine molecules was prepared by microwave activation under mild conditions. Unexpected condensation of isatin derivatives at C-5 position of aminorhodanine was highlighted and confirmed by NMR and X-ray analyses. The inhibitory activity of these compounds was evaluated towards eight protein kinases, CDK's-2,-5,-9; PIM-1, CLK-1, Haspin, GSK3 beta and DYRK1A, whose signaling pathway dysregulation is associated to multifactorial diseases such as cancer, inflammatory, cardiovascular, and neurodegenerative diseases. Compound 3l bearing a bromo substituent has shown a potent and selective Pim1 kinase inhibitor activity. (C) 2019 Elsevier B.V. All rights reserved.