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Targeting Tumor Associated Carbonic Anhydrases IX and XII: Highly Isozyme Selective Coumarin and Psoralen Inhibitors
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-06-06 00:00:00 , DOI: 10.1021/acsmedchemlett.8b00170 Claudia Melis 1 , Simona Distinto 1 , Giulia Bianco 1 , Rita Meleddu 1 , Filippo Cottiglia 1 , Benedetta Fois 1 , Domenico Taverna 2 , Rossella Angius 3 , Stefano Alcaro 4 , Francesco Ortuso 4 , Marco Gaspari 2 , Andrea Angeli 5 , Sonia Del Prete 6 , Clemente Capasso 6 , Claudiu T. Supuran 5 , Elias Maccioni 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-06-06 00:00:00 , DOI: 10.1021/acsmedchemlett.8b00170 Claudia Melis 1 , Simona Distinto 1 , Giulia Bianco 1 , Rita Meleddu 1 , Filippo Cottiglia 1 , Benedetta Fois 1 , Domenico Taverna 2 , Rossella Angius 3 , Stefano Alcaro 4 , Francesco Ortuso 4 , Marco Gaspari 2 , Andrea Angeli 5 , Sonia Del Prete 6 , Clemente Capasso 6 , Claudiu T. Supuran 5 , Elias Maccioni 1
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A small library of psoralen carboxylic acids and their corresponding benzenesulfonamide derivatives were designed and synthesized to evaluate their activity and selectivity toward tumor associated human carbonic anhydrase (hCA) isoforms IX and XII. Both psoralen acids and sulfonamides exhibited potent inhibition of IX and XII isozymes in the nanomolar concentration range. However, psoralen acids resulted as the most selective in comparison with the corresponding benzenesulfonamide derivatives. Our data indicate that the psoralen scaffold is a promising starting point for the design of highly selective tumor associated hCA inhibitors.
中文翻译：
针对肿瘤相关的碳酸酐酶IX和XII：高度同工酶选择性香豆素和补骨脂素抑制剂。
设计并合成了一个小型补骨脂素羧酸文库及其相应的苯磺酰胺衍生物，以评估其对肿瘤相关的人类碳酸酐酶（hCA）亚型IX和XII的活性和选择性。补骨脂酸和磺酰胺在纳摩尔浓度范围内均表现出对IX和XII同功酶的有效抑制作用。然而，补骨脂酸与相应的苯磺酰胺衍生物相比具有最强的选择性。我们的数据表明，补骨脂素支架是设计高度选择性的肿瘤相关hCA抑制剂的有希望的起点。
更新日期：2018-06-06
中文翻译：
针对肿瘤相关的碳酸酐酶IX和XII：高度同工酶选择性香豆素和补骨脂素抑制剂。
设计并合成了一个小型补骨脂素羧酸文库及其相应的苯磺酰胺衍生物，以评估其对肿瘤相关的人类碳酸酐酶（hCA）亚型IX和XII的活性和选择性。补骨脂酸和磺酰胺在纳摩尔浓度范围内均表现出对IX和XII同功酶的有效抑制作用。然而，补骨脂酸与相应的苯磺酰胺衍生物相比具有最强的选择性。我们的数据表明，补骨脂素支架是设计高度选择性的肿瘤相关hCA抑制剂的有希望的起点。
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