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不同含磺酰胺基硫杂环支架的合成及其对碳酸酐酶 II 和 IX 的纳摩尔级抑制作用和 X 射线研究其抑制机制。

Synthesis of different thio-scaffolds bearing sulfonamide with subnanomolar carbonic anhydrase II and IX inhibitory properties and X-ray investigations for their inhibitory mechanism.

机构信息

Department of University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy.

Department of University of Florence, Department of Chemistry "Ugo Schiff", Via della Lastruccia 13, I-50019 Sesto Fiorentino, Italy.

出版信息

Bioorg Chem. 2018 Dec;81:642-648. doi: 10.1016/j.bioorg.2018.09.028. Epub 2018 Sep 20.

DOI:10.1016/j.bioorg.2018.09.028
PMID:30253337
Abstract

Several new molecules with different thio-scaffolds were designed, synthesised, and evaluated biologically as inhibitors of Carbonic Anhydrases (CAIs). The structure-activity relationship analysis identified thioether derivatives, here reported, as a potent and selective CAIs against hCA II and hCA IX. High resolution X-ray structure of inhibitor bound hCA II revealed extensive interactions with the hydrophobic pocket of active site and provided molecular insight into the binding properties of these new inhibitors.

摘要

设计、合成了几种具有不同硫骨架的新分子，并将其作为碳酸酐酶（CAIs）抑制剂进行了生物学评价。构效关系分析确定了硫醚衍生物，本文报道了其作为 hCA II 和 hCA IX 的有效且选择性 CAIs。抑制剂结合的 hCA II 的高分辨率 X 射线结构揭示了与活性位点疏水区的广泛相互作用，并为这些新抑制剂的结合特性提供了分子见解。

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