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

被引:13
|
作者
Gencer, Nahit [1 ]
Bilen, Cigdem [1 ]
Demir, Dudu [1 ]
Atahan, Alparslan [2 ]
Ceylan, Mustafa [3 ]
Kucukislamoglu, Mustafa [4 ]
机构
[1] Balikesir Univ, Fac Art & Sci, Dept Chem, TR-10145 Balikesir, Turkey
[2] Duzce Univ, Fac Art & Sci, Dept Chem, Duzce, Turkey
[3] Gaziosmanpasa Univ, Fac Art & Sci, Dept Chem, Tokat, Turkey
[4] Sakarya Univ, Fac Art & Sci, Dept Chem, Sakarya, Turkey
关键词
carbonic anhydrase; chalcone; urea; thiourea; inhibition; In vitro; UREA DERIVATIVES; BIOLOGICAL EVALUATION; SYNTHETIC CHALCONES; PURIFICATION; FLAVANONES; ANTITUMOR; DESIGN; TARGET; SERIES; DRUGS;
D O I
10.3109/21691401.2012.761226
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
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).
引用
收藏
页码:384 / 388
页数:5
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