The synthesis of axially disubstituted silicon phthalocyanines, their quaternized derivatives and first inhibitory effect on human cytosolic carbonic anhydrase isozymes hCA I and II

Arslan Tayfun; Biyiklioglu Zekeriya; Senturk Murat

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The synthesis of axially disubstituted silicon phthalocyanines, their quaternized derivatives and first inhibitory effect on human cytosolic carbonic anhydrase isozymes hCA I and II

机译：轴向二晶磷酸硅酞菁的合成，其季铵化衍生物及对人胞质碳碳酸酐酶同工酶HCA I和II的第一抑制作用

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In this study a novel silicon(iv) phthalocyanine bearing [(2E)-3-[4-(dimethylamino)phenyl]-1-(4-phenoxy)prop-2-en-1-one] group and its quaternized derivative at their axial positions were synthesized for the first time. Axially disubstituted silicon(iv) phthalocyanines were also characterized by various spectroscopic techniques. The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II, with axially disubstituted silicon phthalocyanines and their quaternized derivatives were investigated by using the esterase assay, with 4-nitrophenyl acetate as substrate. Silicon phthalocyanines ZM-1-Si, ZM-5-Si, ZT-Si and their quaternized derivatives ZM-1-SiQ, ZM-5-SiQ, ZT-SiQ showed IC50 values in the range of 0.0178-0.1653 M for hCA I and of 0.0172-0.1212 M against hCA II, respectively. This study is the first example of carbonic anhydrase enzyme inhibition of phthalocyanines.

机译：在这项研究中，一种新型硅（IV）酞菁轴承[（2E）-3- [4-（二甲基氨基）苯基] -1-（4-苯氧基）prop-2-en-1-one]组及其季铵化衍生物它们的轴向位置是第一次合成。轴向多硅（IV）酞菁的特征在于各种光谱技术。使用酯酶测定法研究了具有轴向二苯酞菁胺和II的两种人胞质碳酸酐酶（HCA，EC 4.2.1.1.1）同工酶I和II的抑制作用。硅酞菁ZM-1-Si，ZM-5-Si，ZT-Si及其季铵化衍生物ZM-1-SiQ，ZM-5-SIQ，ZT-SIQ显示了IC50值，用于HCA I的0.0178-0.1653M 分别对对HCA II的0.0172-0.1212M。该研究是碳酸酐酶抑制酞菁的第一个例子。

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《RSC Advances》 |2018年第19期|共7页
作者
Arslan Tayfun; Biyiklioglu Zekeriya; Senturk Murat;
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Fac Sci Dept Chem Giresun Turkey;

Karadeniz Tech Univ Dept Chem Fac Sci TR-61080 Trabzon Turkey;

Ibrahim Cecen Univ Agri Dept Basic Sci Pharm Fac Pharm TR-04100 Agri Turkey;

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正文语种 eng
中图分类化学;
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1. The synthesis of axially disubstituted silicon phthalocyanines, their quaternized derivatives and first inhibitory effect on human cytosolic carbonic anhydrase isozymes hCA I and II [J] . Arslan Tayfun, Biyiklioglu Zekeriya, Senturk Murat RSC Advances . 2018,第19期

机译：轴向二晶磷酸硅酞菁的合成，其季铵化衍生物及对人胞质碳碳酸酐酶同工酶HCA I和II的第一抑制作用
2. Synthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II) [J] . Altintop Mehlika Dilek, Ozdemir Ahmet, Kucukoglu Kaan, Journal of enzyme inhibition and medicinal chemistry. . 2015,第1a6期

机译：新型噻二唑衍生物的合成和评估作为潜在的人类碳酸酐酶同工酶（hCA-I和hCA-II）
3. Synthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II) [J] . Mehlika Dilek Altintop, Ahmet Ozdemir, Kaan Kucukoglu, Journal of enzyme inhibition and medicinal chemistry. . 2015,第1期

机译：新型噻二唑衍生物的合成和评估作为潜在的人类碳酸酐酶同工酶（hCA-I和hCA-II）
4. Growth and Invasion of Human Cancer Cells: The Roles of Carbonic Anhydrase Isozymes [C] . . 2005

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5. Influence of active site ligands and nanoparticle surfaces on human carbonic anhydrase isozymes. [D] . Manokaran, Sumathra. 2010

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The synthesis of axially disubstituted silicon phthalocyanines, their quaternized derivatives and first inhibitory effect on human cytosolic carbonic anhydrase isozymes hCA I and II

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