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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines
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Pyridazinone-substituted benzenesulfonamides display potent inhibition of membrane-bound human carbonic anhydrase IX and promising antiproliferative activity against cancer cell lines

机译：吡啶酮酮取代的苯磺酰磺酰胺显示出膜结合的人碳酸酐酶IX的有效抑制和对癌细胞系的有希望的抗增殖活性

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摘要

An expanded set of pyridazine-containing benzene sulfonamides was investigated for inhibition of four human carbonic anhydrase isoforms, which revealed a pronounced inhibition trend toward hCA IX, a cancer-related, membrane-bound isoform of the enzyme. Comparison of antiproliferative effects of these compounds against cancer (PANC-1) and normal (ARPE-19) cells at 50 mu M concentration narrowed the selection of compounds to the eight which displayed selective growth inhibition toward the cancer cells. More detailed investigation in concentration-dependent mode against normal (ARPE-19) and two cancer cell lines (PANC-1 and SK-MEL-2) identified two lead compounds one of which displayed a notable cytotoxicity toward pancreatic cancer cells while the other targeted the melanoma cells. These findings significantly expand the knowledge base concerning the hCA IX inhibitors whose inhibitory potency against a recombinant enzyme translates into selective anticancer activity under hypoxic conditions which are aimed to model the environment of a growing tumor. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：研究了一种膨胀的含丙嗪苯磺胺酰胺，用于抑制四种人碳酸酐酶同种型，其揭示了HCA IX的明显抑制趋势，癌症相关的癌症膜结合同种型。将这些化合物对癌症（PANC-1）和正常（ARPE-19）细胞的抗增殖效应的比较在50μmm浓度下将化合物的选择缩小到八个朝向癌细胞的选择性生长抑制。更详细的正常（ARPE-19）和两种癌细胞系（PANK-1和SK-MEL-2）鉴定依赖依赖性模式（PANK-1和SK-MEL-2），其鉴定了两个铅化合物，其中一个铅化合物朝胰腺癌细胞显示出显着的细胞毒性，而另一个靶向黑色素瘤细胞。这些发现显着扩展了关于HCA IX抑制剂的知识基础，其抑制反映酶的效力转化为缺氧条件下的选择性抗癌活性，其旨在模拟生长肿瘤的环境。 （c）2019年Elsevier Masson SAS。版权所有。

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