title: Synthesis and in vitro inhibition effect of new pyrido[2,3-d]pyrimidine derivatives on erythrocyte carbonic anhydrase I and II.
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 CO2 as a substrate. The results showed that all compounds inhibited the hCA I and hCA II enzyme activities. Among all the synthesized compounds, 7e (IC50 = 6.79 µM) was found to be the most active compound for hCA I inhibitory activity and 5 g (IC50 = 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.
authors.affiliation: Department of Chemistry, Faculty of Art and Sciences, Sakarya University, 54140 Sakarya, Turkey.
authors.forename: Hilal
authors.initials: H
authors.lastname: Kuday
authors.affiliation: Pamukova Vocational High School, Sakarya University, 54900 Sakarya, Turkey.
authors.forename: Fatih
authors.initials: F
authors.lastname: Sonmez
authors.affiliation: Department of Chemistry, Faculty of Art and Sciences, Balikesir University, 10145 Balikesir, Turkey.
authors.forename: Cigdem
authors.initials: C
authors.lastname: Bilen
authors.affiliation: Department of Chemistry, Faculty of Art and Sciences, Balikesir University, 10145 Balikesir, Turkey.
authors.forename: Emre
authors.initials: E
authors.lastname: Yavuz
authors.affiliation: Department of Chemistry, Faculty of Art and Sciences, Balikesir University, 10145 Balikesir, Turkey.
authors.forename: Nahit
authors.initials: N
authors.lastname: Gençer
authors.affiliation: Department of Chemistry, Faculty of Art and Sciences, Sakarya University, 54140 Sakarya, Turkey.
authors.forename: Mustafa
authors.initials: M
authors.lastname: Kucukislamoglu
mesh_terms: D002245:Carbon Dioxide / Q000737:chemistry; D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism*; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D002599:Chalcone / Q000008:administration & dosage / Q000138:chemical synthesis*; D004912:Erythrocytes / Q000201:enzymology; D064368:Healthy Volunteers; D006801:Humans; D011743:Pyrimidines / Q000008:administration & dosage / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
chemical_list: D011743:Pyrimidines; D002245:Carbon Dioxide; D002599:Chalcone; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II