一类碳酸酐酶 IX/XII 选择性羧酸酯抑制剂。
A class of carbonic anhydrase IX/XII - selective carboxylate inhibitors.
机构信息
Department of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia.
Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Florence, Italy.
出版信息
J Enzyme Inhib Med Chem. 2020 Dec;35(1):549-554. doi: 10.1080/14756366.2020.1715388.
A small series of 2,4-dioxothiazolidinyl acetic acids was prepared from thiourea, chloroacetic acid, aromatic aldehydes, and ethyl-2-bromoacetate. They were assayed for the inhibition of four physiologically relevant carbonic anhydrase (CA, EC 4.2.1.1) isoforms of human (h) origin, the cytosolic hCA I and II, and the transmembrane hCA IX and XII, involved among others in tumorigenesis (hCA IX and XII) and glaucoma (hCA II and XII). The two cytosolic isoforms were not inhibited by these carboxylates, which were also rather ineffective as hCA IX inhibitors. On the other hand, they showed submicromolar hCA XII inhibition, with Ks in the range of 0.30-0.93 µM, making them highly CA XII-selective inhibitors.
从小系列的 2,4-二氧代噻唑烷-5-乙酸是由硫脲，氯乙酸，芳香醛和溴代乙酸乙酯。他们的抑制四种生理相关碳酸酐酶（CA，EC 4.2.1.1）同工酶的人（H）起源，胞质 hCA I 和 II，和跨膜 hCA 九和十二，除其他外参与肿瘤发生（hCA 九和十二）和青光眼（hCA 二和十二）。这两种胞质同工酶不受这些羧酸的抑制，它们作为 hCA 九抑制剂的效果也相当差。另一方面，它们对 hCA 十二的抑制作用低于亚微摩尔，Ks 值在 0.30-0.93 μM 范围内，使它们成为高度 CA 十二选择性抑制剂。
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