Synthesis and Carbonic Anhydrase I, II, IX, and XII Inhibition Studies with a Series of Cyclic Sulfonyl Guanidines

被引：3

作者：

Abdoli, Morteza ^{[1
]}

Bonardi, Alessandro ^{[2
]}

Supuran, Claudiu T. ^{[2
]}

Zalubovskis, Raivis ^{[1
,3
]}

机构：

[1] Riga Tech Univ, Inst Chem & Chem Technol, Fac Nat Sci & Technol, P Valdena Iela 3, LV-1048 Riga, Latvia

[2] Univ Florence, NEUROFARBA Dept, Pharmaceut & Nutraceut Sect, Via Ugo Schiff 6, I-50019 Florence, Italy

[3] Latvian Inst Organ Synth, Aizkraukles 21, LV-1006 Riga, Latvia

来源：

CHEMMEDCHEM | 2024年 / 19卷 / 19期

关键词：

Carbonic anhydrase inhibitors; Cancer-related isoforms; Antitumor agents; Sulfonamides; Sulfaguanidines; SECONDARY SULFONAMIDES; VII; DERIVATIVES;

D O I：

10.1002/cmdc.202400197

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of thirteen cyclic sulfonyl guanidines were prepared and evaluated against tumor-associated human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA IX and hCA XII, as well as against off-target cytosolic isoforms hCA I and hCA II. The compounds reported here were generally inactive against both off-target isoforms (KI>100 mu M), while all of them moderately inhibited both target isoforms hCA IX and XII in the submicromolar to micromolar ranges in which KI values spanned from 0.57 to 8.4 mu M against hCA IX and from 0.34 to 9.7 against hCA XII. Due to the notable selectivity of the title compounds toward isoforms hCA IX and XII, they can be considered as useful scaffolds for further chemical optimization to develop new highly selective antitumor agents.

引用

页数：7

共 35 条

[21] New superacid synthesized (fluorinated) tertiary benzenesulfonamides acting as selective hCA IX inhibitors: toward a new mode of carbonic anhydrase inhibition by sulfonamides [J].