Synthesis and in vitro inhibition effect of new pyrido[2,3-d]pyrimidine derivatives on erythrocyte carbonic anhydrase i and II
BioMed Research International, vol.2014, 2014 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 2014
- Publication Date: 2014
- Doi Number: 10.1155/2014/594879
- Journal Name: BioMed Research International
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- İstanbul Yeni Yüzyıl University Affiliated: No
Abstract
In vitro inhibition effects of indolylchalcones and new pyrido[2,3-d]pyrimidine derivatives on purified human carbonic anhydrase I and II (hCA I and II) were investigated by using COas a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among all the synthesized compounds, 7e (IC 50 = 6.79 μM) was found to be the most active compound for hCA I inhibitory activity and 5g (IC 50 = 7.22 μM) showed the highest hCA II inhibitory activity. Structure-activity relationships study showed that indolylchalcone derivatives have higher inhibitory activities than pyrido[2,3-d]pyrimidine derivatives on hCA I and hCA II. Additionally, methyl group bonded to uracil ring increases inhibitory activities on both hCA I and hCA II.