通过5个步骤从商业上可获得的水杨醛合成了一系列在框架的7号、8号或9号位置具有各种取代模式的3H-1,2-苯氧磷庚酮芳基衍生物。对所有新获得的化合物进行了对碳酸酐酶（CA）亚型I、II、IX和XII的抑制效力的研究。令人欣喜的是，这些化合物对于与癌症相关的CA IX和XII表现出显著的选择性，而对细胞质CA I和II的抑制可能导致副作用。总体而言，结构-活性关系（SAR）揭示了7-和8-取代的芳基衍生物对于抑制CA IX和XII的效果比9-取代的衍生物更有效。此外，这一系列化合物中含氟的类似物表现出最强的CA IX/XII抑制剂活性。

A range of 3H-1,2-benzoxaphosphepine 2-oxide aryl derivatives with various substitution patterns at positions 7, 8, or 9 of the scaffold was synthesised in five steps from the commercially available salicylaldehydes. All of the newly obtained compounds were studied for their inhibition potency against carbonic anhydrase (CA) isoforms I, II, IX, and XII. Delightfully, these compounds showed a striking selectivity for the cancer-associated CA IX and XII over the cytosolic CA I and II, whose inhibition may lead to side-effects. Overall, a structure-activity relationship (SAR) revealed that 7- and 8-substituted aryl derivatives were more effective inhibitors of CA IX and XII than 9-substituted derivatives. In addition, the fluorine-containing analogues emerged as the most potent CA IX/XII inhibitors in this series.