Experimental Carbonic Anhydrase Inhibitors for the Treatment of Hypoxic Tumors

Figures & data

Figure 1 Fluorescent inhibitors 1, 2 used to validate hCA IX/XII as antitumor drug targets^60–63 and the pan-inhibitor acetazolamide 3.

Figure 2 Acetazolamide-based CAIs 4, 5 and 7 reported by Neri’s group and the cytotoxin 6 (DM1).^64,66

Figure 3 Nitroazole-containing CAIs of types 8–11.^74–79

Figure 4 Sulfamates incorporating ureido (compounds 12, 14 and 15) and thioureido (13) moieties, with effective CA IX/XII inhibitory action and investigated for their antitumor effects. S4 was the most extensively investigated such derivative.⁸⁰

Figure 5 Examples of glycomimetic CAIs incorporating benzenesulfonamide, sugar and 1,2,3-triazole moieties, of types 16–22.^82–89

Figure 6 The natural product sulfonamide Psammaplin C, 23.⁹⁶

Figure 7 Ureido-sulfonamides 24 and 25 and 7-glycosyl-substituted coumarins 26, 27.^98–101

Figure 8 Sulfonamides 28–43 designed as anti-cancer derivatives using SLC-0111 as lead molecule.

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