Organoruthenium(II) complexes of acetazolamide potently inhibit human carbonic anhydrase isoforms I, II, IX and XII

Figures & data

Figure 1. Clinically used sulfonamides with CA inhibitory activity^1–3.

Figure 2. Structure of acetazolamide organoruthenium complexes 1 (left) and 2 (right). The X-ray crystallography for these compounds was reported in Biancalana et al.¹⁸

Table 1. Inhibition of human (h) CA isoforms hCA I, II, IX and XII with acetazolamide (AAZ) and its two Ru(II) derivatives 1 and 2, by a stopped flow, CO₂ hydrase assay.

	KI (nM)*
Compound	hCA I	hCA II	hCA IX	hCA XII
AAZ	250	12.0	25.2	5.7
1	23.4	4.2	3.8	0.52
2	8.5	0.48	0.63	0.04

* Mean from three different assays. Errors were in the range of ±5%–10% of the reported values (data not shown).

Biancalana L, Batchelor LK, Ciancaleoni G, et al. Versatile coordination of acetazolamide to ruthenium(II) p-cymene complexes and preliminary cytotoxicity studies. Dalton Trans 2018;47:9367–84.

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