A series of N′-phenyl-N-hydroxyureas has been prepared by reacting hydroxylamine with aromatic isocyanates. These compounds were investigated as inhibitors of human carbonic anhydrases (hCAs, EC 4.2.1.1), considering four physiologically relevant isoforms, the cytosolic isoforms hCA I and II, and tumor associated, transmembrane isoforms hCA IX and XII. The new compounds reported here did not inhibit the widespread cytosolic isoforms hCA I and II, but they inhibited the tumor associated isoforms with interesting potencies. The most effective inhibitors showed K_Is ranging between 72.8 and 78.9 nM against hCA IX and between 6.9 and 7.2 against hCA XII, making them of interest as candidates for antitumor studies.

通过使羟胺与芳族异氰酸酯反应，制备了一系列的N'-苯基-N-羟基脲。研究了这些化合物作为人类碳酸酐酶（hCAs，EC 4.2.1.1）的抑制剂，考虑了四种生理相关的同工型，即胞质同工型hCA I和II，以及与肿瘤相关的跨膜同工型hCA IX和XII。此处报道的新化合物并未抑制广泛的胞质亚型hCA I和II，但它们以令人感兴趣的效力抑制了与肿瘤相关的亚型。最有效的抑制剂显示出针对hCA IX的K _I介于72.8至78.9 nM之间，针对hCA XII的K _I在6.9至7.2 nM之间，使其成为抗肿瘤研究的候选对象。