a Department of Drug Radiation Research, National Center for Radiation Research and Technology (NCRRT) , Egyptian Atomic Energy Authority (EAEA) , Cairo , Egypt.
b NEUROFARBA Department, Pharmaceutical and Nutraceutical Sciences Section , University of Florence , Firenze , Italy.
J Enzyme Inhib Med Chem. 2018 Dec;33(1):1565-1574. doi: 10.1080/14756366.2018.1513927.
We report the synthesis and characterisation of a novel series of triazole benzenesulfonamide derivatives, which incorporate the general pharmacophore associated with carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The synthesised compounds were tested in vitro against four human carbonic anhydrase (hCA, EC 4.2.1.1) isozymes, hCA I, hCA II, hCA IV and hCA IX. The obtained results showed that the tumour-associated hCA IX was the most sensitive to inhibition with the synthesised derivatives, with the triazolo-pyridine benzenesulfonamides 14, 16 and 17 being the most effective inhibitors. Some selected compounds were chosen for a single dose anti-proliferative activity testing against a panel of 57 human tumour cell lines and show some anti-proliferative activity ex vivo.
我们报告了一系列新型三唑苯磺酰胺衍生物的合成和表征，这些衍生物包含与碳酸酐酶（CA，EC 4.2.1.1）抑制剂相关的一般药效团。合成的化合物在体外针对四种人碳酸酐酶（hCA，EC 4.2.1.1）同工酶 hCA I、hCA II、hCA IV 和 hCA IX 进行了测试。获得的结果表明，与肿瘤相关的 hCA IX 对合成衍生物的抑制最为敏感，三唑并吡啶苯磺酰胺 14、16 和 17 是最有效的抑制剂。选择一些选定的化合物进行了单次剂量抗增殖活性测试，针对 57 个人类肿瘤细胞系panel，并显示出一些体外抗增殖活性。
