Tags

Type your tag names separated by a space and hit enter

Organoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XII.
J Enzyme Inhib Med Chem. 2019 Dec; 34(1):388-393.JE

Abstract

Two acetazolamide (AAZ) complexes with ruthenium(II) η6-p-cymene chloride were synthesised, characterised and tested for their inhibitory effects on several carbonic anhydrase (CA, EC 4.2.1.1) isoforms with pharmacological applications. Against human (h) isoform hCA I, the two complexes showed inhibition constants in the range of 8.5-23.4 nM (AAZ has a KI of 250 nM), against hCA II of 0.48-4.2 nM, whereas against hCA IX of 0.63-3.8 nM and against hCA XII of 0.04-0.52 nM, respectively. These highly effective ruthenium acetazolamide derivatives against the tumour-associated CA isoforms IX and XII warrant further in vivo studies, in hypoxic tumours overexpressing these enzymes.

Authors+Show Affiliations

a Faculty of Chemistry and Chemical Technology , University of Ljubljana , Ljubljana , Slovenia.a Faculty of Chemistry and Chemical Technology , University of Ljubljana , Ljubljana , Slovenia.a Faculty of Chemistry and Chemical Technology , University of Ljubljana , Ljubljana , Slovenia.a Faculty of Chemistry and Chemical Technology , University of Ljubljana , Ljubljana , Slovenia.b Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Florence , Italy.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30734595

Citation

Seršen, Sara, et al. "Organoruthenium(II) Complexes of Acetazolamide Potently Inhibit Human Carbonic Anhydrase Isoforms I, II, IX and XII." Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 34, no. 1, 2019, pp. 388-393.
Seršen S, Traven K, Kljun J, et al. Organoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XII. J Enzyme Inhib Med Chem. 2019;34(1):388-393.
Seršen, S., Traven, K., Kljun, J., Turel, I., & Supuran, C. T. (2019). Organoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XII. Journal of Enzyme Inhibition and Medicinal Chemistry, 34(1), 388-393. https://doi.org/10.1080/14756366.2018.1547288
Seršen S, et al. Organoruthenium(II) Complexes of Acetazolamide Potently Inhibit Human Carbonic Anhydrase Isoforms I, II, IX and XII. J Enzyme Inhib Med Chem. 2019;34(1):388-393. PubMed PMID: 30734595.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Organoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XII. AU - Seršen,Sara, AU - Traven,Katja, AU - Kljun,Jakob, AU - Turel,Iztok, AU - Supuran,Claudiu T, PY - 2019/2/9/entrez PY - 2019/2/9/pubmed PY - 2019/3/15/medline KW - Carbonic anhydrase KW - Ru(II) KW - acetazolamide KW - human isoforms KW - metal complex SP - 388 EP - 393 JF - Journal of enzyme inhibition and medicinal chemistry JO - J Enzyme Inhib Med Chem VL - 34 IS - 1 N2 - Two acetazolamide (AAZ) complexes with ruthenium(II) η6-p-cymene chloride were synthesised, characterised and tested for their inhibitory effects on several carbonic anhydrase (CA, EC 4.2.1.1) isoforms with pharmacological applications. Against human (h) isoform hCA I, the two complexes showed inhibition constants in the range of 8.5-23.4 nM (AAZ has a KI of 250 nM), against hCA II of 0.48-4.2 nM, whereas against hCA IX of 0.63-3.8 nM and against hCA XII of 0.04-0.52 nM, respectively. These highly effective ruthenium acetazolamide derivatives against the tumour-associated CA isoforms IX and XII warrant further in vivo studies, in hypoxic tumours overexpressing these enzymes. SN - 1475-6374 UR - https://www.unboundmedicine.com/medline/citation/30734595/Organoruthenium_II__complexes_of_acetazolamide_potently_inhibit_human_carbonic_anhydrase_isoforms_I_II_IX_and_XII_ L2 - https://www.tandfonline.com/doi/full/10.1080/14756366.2018.1547288 DB - PRIME DP - Unbound Medicine ER -