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European journal of medicinal chemistry

Carbonic anhydrase inhibitors-Part 94. 1, 3, 4-Thiadiazole-2-sulfonamide derivatives as antitumor agents?

CT Supuran, A Scozzafava

文献索引:Scozzafava, Andrea; Supuran, Claudiu T. European Journal of Medicinal Chemistry, 2000 , vol. 35, # 1 p. 31 - 39

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被引用次数: 140

摘要

Potent sulfonamide inhibitors of the zinc enzyme carbonic anhydrase (CA, EC 4.2. 1.1), derivatives of 1, 3, 4-thiadiazole-2-sulfonamide, possessing inhibition constants in the range of 10–8–10–9 M against isozymes II and IV, were shown to act as efficient in vitro tumour cell growth inhibitors with GI50 (molarity of inhibitor producing a 50% inhibition of tumour cell growth) values typically in the range of 0.1–30 μM against several leukaemia, non-small ...