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新型含磺酰胺基的2-吲哚酮类化合物，其可选择性抑制肿瘤相关的α-碳酸酐酶。

Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases.

作者信息

Karalı Nilgün, Akdemir Atilla, Göktaş Füsun, Eraslan Elma Pınar, Angeli Andrea, Kızılırmak Merih, Supuran Claudiu T

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul 34116, Turkey.

Computer-Aided Drug Discovery Laboratory, Department of Pharmacology, Faculty of Pharmacy, Bezmialem Vakif University, Istanbul 34093, Turkey.

出版信息

Bioorg Med Chem. 2017 Jul 15;25(14):3714-3718. doi: 10.1016/j.bmc.2017.05.029. Epub 2017 May 15.

DOI:10.1016/j.bmc.2017.05.029
PMID:28545816
Abstract

Human carbonic anhydrases IX and XII are upregulated in many tumors and form a novel target for new generation anticancer drugs. Here we report the synthesis of novel 2-indolinone derivatives with the sulfonamide group as a zinc binding moiety. Enzyme inhibition assays confirmed that the compounds showed selectivity against hCA IX and XII over the widely distributed off-targets hCA I and II. Molecular modelling studies were performed to suggest modes of binding for these compounds.

摘要

人类碳酸酐酶IX和XII在许多肿瘤中上调，并成为新一代抗癌药物的新靶点。在此，我们报道了以磺酰胺基团作为锌结合部分的新型2-吲哚酮衍生物的合成。酶抑制试验证实，这些化合物对hCA IX和XII具有选择性，优于广泛分布的脱靶酶hCA I和II。进行了分子模拟研究以推测这些化合物的结合模式。

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