5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII.

doi:10.1016/j.bmc.2015.05.052

Paper

5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII.

Published Aug 1, 2015 · Ilija N. Cvijetić, Muhammet Tanc, I. Juranić

Bioorganic & medicinal chemistry

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Abstract

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In Vitro Study

Study Snapshot

Selective inhibition of human carbonic anhydrase IX and XII by 5-aryl-1H-pyrazole-3-carboxylic acids could lead to the development of isoform-specific non-sulfonamide CA inhibitors.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII.

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References

Citations

Inherent efficacies of pyrazole-based derivatives for cancer therapy: the interface between experiment and in silico.

Pyrazole-based derivatives show promise for cancer therapy when combined with experimental and computational methods, targeting key targets like tubulin polymerization, carbonic anhydrase, and tyrosine kinase.

Design, synthesis, in vitro and in silico evaluation of anti-colorectal cancer activity of curcumin analogues containing 1,3-diphenyl-1H-pyrazole targeting EGFR tyrosine kinase.

Curcumin analogues containing 1,3-diphenyl-1H-pyrazole show promising anti-colorectal cancer activity by targeting EGFR tyrosine kinase and inducing apoptosis in cancer cells.

A novel class of phenylpyrazolone-sulphonamides rigid synthetic anticancer molecules selectively inhibit the isoform IX of carbonic anhydrases guided by molecular docking and orbital analyses

Novel phenylpyrazolone-sulphonamides with sulfonamide head and aryl hydrophobic tail show potential as selective inhibitors of human carbonic anhydrases, showing good cytotoxic activities against breast and colorectal carcinomas.

Dependence on linkers’ flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents

Compounds 5d and 13c show significant anticancer activity, while 13c shows positive effects on normal cell lines, metastasis, and wound healing.

Synthesis, Biological Evaluation, and Molecular Modeling Studies of 1-Aryl-1H-pyrazole-Fused Curcumin Analogues as Anticancer Agents

Curcumin analogues synthesized in this study show potential as anticancer agents, with compounds 7d, 7h, and 10c showing microtubule-destabilizing effects and apoptosis-inducing activities in breast cancer MDA-MB-231 cells.