Novel 1,2,4-triazoles as selective carbonic anhydrase inhibitors showing ancillary anticathepsin B activity
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - year:2024 |
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| Enthalten in: |
Future medicinal chemistry - (2024) vom: 04. Apr. |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Kumar, Amit [VerfasserIn] |
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| Links: |
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| Themen: |
1,2,4-triazole |
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| Anmerkungen: |
Date Revised 04.04.2024 published: Print-Electronic Citation Status Publisher |
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| doi: |
10.4155/fmc-2023-0321 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM370624467 |
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| 100 | 1 | |a Kumar, Amit |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Novel 1,2,4-triazoles as selective carbonic anhydrase inhibitors showing ancillary anticathepsin B activity |
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| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a benzenesulfonamide | |
| 650 | 4 | |a cancer | |
| 650 | 4 | |a carbonic anhydrase inhibitors | |
| 650 | 4 | |a cathepsin B inhibitors | |
| 650 | 4 | |a tail-approach | |
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| 700 | 1 | |a Giovannuzzi, Simone |e verfasserin |4 aut | |
| 700 | 1 | |a Mohan, Brij |e verfasserin |4 aut | |
| 700 | 1 | |a Raghav, Neera |e verfasserin |4 aut | |
| 700 | 1 | |a Supuran, Claudiu T |e verfasserin |4 aut | |
| 700 | 1 | |a Sharma, Pawan K |e verfasserin |4 aut | |
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