A series of benzenesulfonamides bearing selenourea moieties was obtained considering the ureido-sulfonamide SLC-0111, in Phase I clinical trials as antitumor agent, as a lead molecule. All compounds showed interesting inhibition potencies against the physiologically relevant human (h) carbonic anhydrase (hCAs, EC 4.2.1.1) isoforms I, II, IV, and IX. The most flexible analogues in the series 14–19 showed low nanomolar inhibition constants against hCA I, II, and IX. We assessed selected compounds on the in vitro antioxidant properties and binding modes and evaluated ex vivo human prostate (PC3), breast (MDA-MB-231), and colon-rectal (HT-29) cancer cell lines both in normoxic and hypoxic conditions.

中文翻译：

---

作为碳酸酐酶抑制剂的 4-(4-氟苯基脲基)苯磺酰胺的新硒脲基类似物的发现

以脲基磺酰胺SLC-0111为先导分子，在I期临床试验中作为抗肿瘤剂，获得了一系列带有硒脲部分的苯磺酰胺。所有化合物均对生理相关的人 (h) 碳酸酐酶 (hCAs，EC 4.2.1.1) 亚型 I、II、IV 和 IX 表现出有趣的抑制效力。系列14 – 19中最灵活的类似物对 hCA I、II 和 IX 表现出低纳摩尔抑制常数。我们评估了选定化合物的体外抗氧化特性和结合模式，并评估了常氧和缺氧条件下的离体人前列腺 (PC3)、乳腺癌 (MDA-MB-231) 和结肠直肠 (HT-29) 癌细胞系。