University of Florence, NEUROFARBA Department, Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
Chem Commun (Camb). 2019 Jan 10;55(5):648-651. doi: 10.1039/c8cc08562e.
Stable aryl selenols were obtained through a convenient procedure. Selenols represent a new chemotype acting as carbonic anhydrase inhibitors (CAIs), inhibiting four human isoforms, CAs I, II, VII and the tumor-associated CA IX. X-ray crystallographic, physical and computational studies provided insights into the binding mode of this conceptually new class of CAIs.
稳定的芳基硒醇是通过一种简便的方法得到的。硒醇代表了一种新的化学型,作为碳酸酐酶抑制剂(CAIs),抑制四种人同工酶,即 CA I、CA II、CA VII 和与肿瘤相关的 CA IX。X 射线晶体学、物理和计算研究提供了对这种新概念 CAIs 结合模式的深入了解。