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. 2012 Jan 28;3(1):84–97. doi: 10.18632/oncotarget.422

Table 2. Targeting of CAIX by small molecules in preclinical models of human cancer.

Tumor Model [citation] Inhibitor Effect
LS174T human colon carcinoma [109] fluoro-acetazolamide bound to xenograft tissue; no significant effect on tumor growth
SK-RC-52 human renal cell carcinoma [109] albumin-acetazolamide significant reduction in tumor growth
HT-29 human renal cell carcinoma [110] bis sulfonamide tumor-specific accumulation; effect on tumor growth not measured
HT-29 human renal cell carcinoma [111] fluorescent sulfonamide tumor-specific accumulation; effect on tumor growth not measured
4T1 metastatic mouse breast cancer [23] fluorescent sulfonamide significant inhibition of tumor growth
4T1 metastatic mouse breast cancer [23, 102] ureido sulfonamides inhibition of experimental lung metastases
4T1 metastatic mouse breast cancer [23, 103] glycosyl coumarins inhibition of experimental lung metastases; inhibition of primary tumor growth
MDA-MB-231 LM2-4 lung metastatic breast cancer [23] ureido sulfonamides inhibition of primary tumor growth
HT-29 human renal cell carcinoma [84] indanesulfonamide inhibition of primary tumor growth; synergy with radiotherapy