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 -