Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors

被引：20
|
作者：
Rosatelli, Emiliano [1 ]
Carotti, Andrea [1 ]
Ceruso, Mariangela [2 ]
Supuran, Claudiu T. [3 ]
Gioiello, Antimo [1 ]
机构：
[1] Univ Perugia, Dept Pharmaceut Sci, Lab Med & Adv Synthet Chem Lab MASC, I-06123 Perugia, Italy
[2] Univ Florence, Lab Bioinorgan Chem, I-50019 Florence, Italy
[3] Univ Florence, Sect Pharmaceut & Nutriceut Sci, Neurofarba Dept, I-50019 Florence, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 15期
关键词：
Carbonic anhydrases; Flow synthesis; Sulfonamides; Docking;
D O I：
10.1016/j.bmcl.2014.05.086
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of secondary and tertiary aryl sulfonamides were synthesized under flow conditions and evaluated for their ability to selectively inhibit tumor-associated carbonic anhydrase isoforms IX and XII. The tested compounds revealed to be highly potent CA IX inhibitors in nanomolar range, and to inhibit CA XII activity with different ranks of potencies. Remarkably, 4-methyl-N-phenyl-benzenesulfonamide was a selective nanomolar CA IX inhibitor with an IC50 of 90 nM. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3422 / 3425
页数：4
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