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磺胺衍生物对碳酸酐酶 II 的抑制作用。

Inhibition of carbonic anhydrase II by sulfonamide derivatives.

机构信息

College of Chemical Engineering, Qingdao University of Science & Technology, Qingdao, PR China.

College of Chemical Engineering, Qingdao University of Science & Technology, Qingdao, PR China;, Email:

出版信息

Pharmazie. 2021 Sep 1;76(9):412-415. doi: 10.1691/ph.2021.1590.

Abstract

A series of sulfonamide derivatives were synthesized, and the enzyme inhibitory activity of the synthesized compounds on carbonic anhydrase II was evaluated. Through molecular docking studies, it was found that compounds , , , , have a strong binding affinity to carbonic anhydrase II. The IC values of the four compounds , , , and were lower than that of the positive control drug acetazolamide. What's more, the compounds had a high inhibitory activity for A549 lung cancer cell growth, among them, and could inhibit both carbonic anhydrase II and lung cancer cell proliferation.

摘要

合成了一系列磺胺衍生物,并评价了它们对碳酸酐酶 II 的抑制活性。通过分子对接研究发现,化合物 、 、 、 与碳酸酐酶 II 具有较强的结合亲和力。化合物 、 、 、 的 IC 值均低于阳性对照药乙酰唑胺。此外,这些化合物对 A549 肺癌细胞生长具有较高的抑制活性,其中 、 可同时抑制碳酸酐酶 II 和肺癌细胞增殖。

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