芳基磺酰胺作为选择性碳酸酐酶IX和XII抑制剂的流动合成及生物活性
Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors.
作者信息
Rosatelli Emiliano, Carotti Andrea, Ceruso Mariangela, Supuran Claudiu T, Gioiello Antimo
机构信息
Laboratory of Medicinal and Advanced Synthetic Chemistry (Lab MASC), Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, Perugia I-06123, Italy.
Laboratory of Bioinorganic Chemistry, University of Florence, Via della Lastruccia 3, Sesto Fiorentino (Firenze) I-50019, Italy.
出版信息
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3422-5. doi: 10.1016/j.bmcl.2014.05.086. Epub 2014 Jun 4.
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.
在流动条件下合成了一系列仲芳基和叔芳基磺酰胺，并评估了它们选择性抑制肿瘤相关碳酸酐酶同工型IX和XII的能力。测试的化合物显示在纳摩尔范围内是高效的CA IX抑制剂，并以不同的效价等级抑制CA XII活性。值得注意的是，4-甲基-N-苯基苯磺酰胺是一种选择性纳摩尔CA IX抑制剂，IC50为90 nM。
Zotero 插件