In vitro inhibition effect of some chalcones on erythrocyte carbonic anhydrase I and II

Gencer N., Bilen C., Demir D., Atahan A., Ceylan M., Kucukislamoglu M.

ARTIFICIAL CELLS NANOMEDICINE AND BIOTECHNOLOGY, vol.41, no.6, pp.384-388, 2013 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 41 Issue: 6
  • Publication Date: 2013
  • Doi Number: 10.3109/21691401.2012.761226
  • Journal Name: ARTIFICIAL CELLS NANOMEDICINE AND BIOTECHNOLOGY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.384-388
  • Keywords: carbonic anhydrase, chalcone, urea, thiourea, inhibition, In vitro, UREA DERIVATIVES, BIOLOGICAL EVALUATION, SYNTHETIC CHALCONES, PURIFICATION, FLAVANONES, ANTITUMOR, DESIGN, TARGET, SERIES, DRUGS
  • Yıldız Technical University Affiliated: No

Abstract

In this study, 4'-(phenylurenyl/thiourenyl) chalcones (14-25) were prepared from 4'-(phenylurenyl/thiourenyl)acetophenones and benzaldehyde derivatives by Claisen-Schmidt condensation. In vitro inhibition effects of chalcone derivatives on purified carbonic anhydrase I and carbonic anhydrase II were investigated by using the CO2 hydration method of Maren. The result showed that all the synthesized compounds inhibited the CA isoenzymes activity. 18 and 19 were found to be most active (IC50 = 25.41 m M and 23.06 mu M) for hCA I, respectively. For hCA II, 24 is the most active compound (IC50 = 14.40 mu M).