Department of Life and Environmental Sciences, University of Cagliari, Monserrato, Italy.
Dipartimento di Scienze della Salute, Università Magna Graecia di Catanzaro, Catanzaro, Italy.
J Enzyme Inhib Med Chem. 2021 Dec;36(1):685-692. doi: 10.1080/14756366.2021.1887171.
A small library of coumarin and their psoralen analogues and has been designed and synthesised to investigate the effect of structural modifications on their inhibition ability and selectivity profile towards carbonic anhydrase isoforms I, II, IX, and XII. None of the new compounds exhibited activity towards hCA I and II isozymes. Conversely, both coumarin and psoralen derivatives were active against tumour associated isoforms IX and XII in the low micromolar or nanomolar range of concentration. These data further corroborate our previous findings on analogous derivatives, confirming that both coumarins and psoralens are interesting scaffolds for the design of isozyme selective hCA inhibitors.
已经设计并合成了一个香豆素及其补骨脂素类似物的小文库,以研究结构修饰对其抑制能力和对碳酸酐酶同工酶 I、II、IX 和 XII 的选择性特征的影响。新化合物均对 hCA I 和 II 同工酶没有活性。相反,香豆素和补骨脂素衍生物对低微摩尔或纳摩尔浓度范围内的肿瘤相关同工酶 IX 和 XII 均具有活性。这些数据进一步证实了我们之前对类似衍生物的发现,证实香豆素和补骨脂素都是设计同工酶选择性 hCA 抑制剂的有趣支架。