Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles

KOÇYİĞİT Ü. M. , Budak Y., Gurdere M. B. , Erturk F., Yencilek B., Taslimi P., ...Daha Fazla

ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY, cilt.124, sa.1, ss.61-68, 2018 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 124 Konu: 1
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1080/13813455.2017.1360914
  • Sayfa Sayıları: ss.61-68


The new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5a-g) were prepared from 4-aminchalcones (3a-g) and screened for biological activities. All compounds (3a-g and 5a-g), except 3d and 3e displayed good cytotoxic activities with IC50 values in the range of 7.06-67.46 mu M. IC50 value of 5-fluorouracil (5-FU) was 90.36 mu M. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25mm of Sulbactam-Cefoperazone (SCF)). In addition, they showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase I, and II (hCA I and hCA II) isoforms. Also, these compounds demonstrated effective inhibition profiles with Ki values of 426.47-699.58 nM against hCA I, 214.92-532.21 nM against hCA II, and 70.470-229.42nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 +/- 227.4nM against CA I, and 904.47 +/- 106.3 nM against CA II, respectively. Also, tacrine inhibited AChE showed a Ki value of 446.56 +/- 58.33 nM.