Novel coumarins and benzocoumarins acting as isoform-selective inhibitors against the tumor-associated carbonic anhydrase IX

Figures & data

Table 1. hCA I, II, IX and XII inhibition data with coumarins 1–5 by a stopped flow, CO₂ hydrase assay31.

		Ki (µM)*
Compounds	hCA I	hCA II	hCA IX	hCA XII
1	4.8	>200	0.45	4.3
2	8.4	>200	0.19	6.4
3	8.7	>200	0.27	6.6
4	9.0	>200	0.23	5.5
5	8.2	>200	0.20	3.3

*Mean from three different assays, errors in the range of ±10% of the reported values.

Scheme 1. Preparation of the coumarins/benzocoumarins 1–5 from phenols A, C and D and ethyl acetoacetate B.

Khalifah RG. The carbon dioxide hydration activity of carbonic anhydrase. I. Stop-flow kinetic studies on the native human isoenzymes B and C. J Biol Chem 1971;246:2561–73

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