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| http://dx.doi.org/10.1042/bj0550696 | DOI Listing |
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Sulphonyl thiourea compounds containing pyrimidine as dual inhibitors of I, II, IX, and XII carbonic anhydrases and cancer cell lines: synthesis, characterization and studies.
RSC Med Chem
December 2024
VNU University of Education, Vietnam National University, Hanoi 144 Xuan Thuy, Cau Giay Ha Noi Vietnam.
Some novel sulphonyl thiourea derivatives (7a-m) containing 4,6-diarylpyrimidine rings were designed and synthesized using a one-pot procedure. These compounds exhibited remarkable dual inhibitory activity against human carbonic anhydrase CA I, CA II, CA IX, and XII isoenzymes and some cancer cell lines. Among them, some thioureas had significantly more potent inhibitory activities in the order of 7l > 7c > 7f (against the CA I isoform), 7f > 7b > 7c (against the CA II isoform), 7c > 7g > 7a > 7b (against the CA IX isoform), and 7d > 7c > 7g > 7f (against the CA XII isoform).
View Article and Find Full Text PDFTetrazole Is a Novel Zinc Binder Chemotype for Carbonic Anhydrase Inhibition.
ACS Med Chem Lett
January 2025
NEUROFARBA Department, Section of Pharmaceutical Science, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
The tetrazole group is here proposed as a zinc-binding warhead for the inhibition of the metalloenzyme carbonic anhydrases. A set of synthesized derivatives incorporating the tetrazole moiety were evaluated as inhibitors against a panel of human isoforms, exhibiting values spanning between the submicromolar and low-to-medium micromolar ranges (0.62-19.
View Article and Find Full Text PDFCopper-based biomimetic nanozymes with multi-enzyme activity for phosphate detection.
Spectrochim Acta A Mol Biomol Spectrosc
December 2024
National Engineering Laboratory for AIDS Vaccine, Key Laboratory for Molecular Enzymology and Engineering, The Ministry of Education, School of Life Sciences, Jilin University, Changchun 130012, China. Electronic address:
Nanozymes are nanoparticles with enzymatic activity, which are widely used in environmental and antibacterial research. Herein, we designed and synthesized novel amorphous nanozyme Cu-Im NPs with multiple enzyme-mimicking activities. Cu-Im NPs have the same active sites as natural laccase.
View Article and Find Full Text PDFMultiple Binding Modes of Inhibitors to Human Carbonic Anhydrases: An Update on the Design of Isoform-Specific Modulators of Activity.
Chem Rev
January 2025
Institute of Biostructures and Bioimaging-CNR, via Pietro Castellino 111, 80131 Naples, Italy.
Human carbonic anhydrases (hCAs) are widespread zinc enzymes that catalyze the hydration of CO to bicarbonate and a proton. Currently, 15 isoforms have been identified, of which only 12 are catalytically active. Given their involvement in numerous physiological and pathological processes, hCAs are recognized therapeutic targets for the development of inhibitors with biomedical applications.
View Article and Find Full Text PDFThe Antiepileptic Drug Levetiracetam Inhibits Carbonic Anhydrase: and Studies on Catalytically Active Human Isoforms.
ACS Med Chem Lett
December 2024
NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, University of Florence, Sesto Fiorentino, 50019 Florence Italy.
Several antiepileptic drugs (AEDs) have been found to inhibit human carbonic anhydrases (hCAs), paving the way for repurposing AEDs for the treatment of various diseases, including cancer. Here, the hCAs inhibitory effects of levetiracetam, a highly prescribed AED that does not bear a common zinc-binding group, were investigated and . Levetiracetam inhibited all tested hCAs, although with a specific profile compared to the reference acetazolamide, with remarkable efficacy against tumor-associated hCA IX and XII.
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