Novel 1,2,4-triazoles as selective carbonic anhydrase inhibitors showing ancillary anticathepsin B activity

被引：2
作者：
Kumar, Amit [1 ]
Arya, Priyanka [1 ]
Giovannuzzi, Simone [2 ]
Mohan, Brij [3 ]
Raghav, Neera [1 ]
Supuran, Claudiu T. [2 ]
Sharma, Pawan K. [1 ,4 ]
机构：
[1] Kurukshetra Univ, Dept Chem, Kurukshetra 136119, Haryana, India
[2] Univ Florence, Neurofarba Dept, Pharmaceut & Nutraceut Sect, I-50139 Florence, Italy
[3] Univ Lisbon, Inst Mol Sci, Ctr Quim Estrutural, Inst Super Tecn, Av Rovisco Pais, P-1049001 Lisbon, Portugal
[4] Cent Univ Haryana, Dept Chem, Mahendergarh 123031, Haryana, India
来源：
FUTURE MEDICINAL CHEMISTRY | 2024年 / 16卷 / 08期
关键词：
1,2,4-triazole; benzenesulfonamide; cancer; carbonic anhydrase inhibitors; cathepsin B inhibitors; tail-approach; CATHEPSIN-B; ISOFORMS I; SULFONAMIDES; GROWTH; TRANSMEMBRANE; DERIVATIVES; DESIGN; TARGET; XII;
D O I：
10.4155/fmc-2023-0321
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Background: Exploration of the multi-target approach considering both human carbonic anhydrase (hCA) IX and XII and cathepsin B is a promising strategy to target cancer. Methodology & Results: 22 novel 1,2,4-triazole derivatives were synthesized and evaluated for their inhibition efficacy against hCA I, II, IX, XII isoforms and cathepsin B. The compounds demonstrated effective inhibition against hCA IX and/or XII isoforms with considerable selectivity over off-target hCA I/II. All compounds presented significant anticathepsin B activities at a low concentration of 10(-7) M and in vitro results were also supported by the molecular modeling studies. Conclusion: Insights of present study can be utilized in the rational design of effective and selective hCA IX and XII inhibitors capable of inhibiting cathepsin B. [GRAPHICS] .
引用
收藏
页码：689 / 706
页数：18
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