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7, 8-Disubstituted-but not 6, 7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and XII over the …

A Maresca, A Scozzafava, CT Supuran

文献索引:Maresca, Alfonso; Scozzafava, Andrea; Supuran, Claudiu T. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7255 - 7258

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被引用次数: 78

摘要

Two series of disubstituted coumarins incorporating ether and acetyl/propionyl moieties in positions 6, 7-and 7, 8-of the heterocyclic ring were synthesized investigated for the inhibition of the zinc enzyme carbonic anhydrase (CA, EC 4.2. 1.1). All these coumarins were very weak or ineffective as inhibitors of the housekeeping, offtarget isoforms CA I and II. The 6, 7-disubstituted series showed ineffective inhibition also for the transmembrane ...