Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV.

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Scozzafava A, Supuran CT

Carbonic anhydrase inhibitors: synthesis of N-morpholylthiocarbonylsulfenylamino aromatic/heterocyclic sulfonamides and their interaction with isozymes I, II and IV.

Bioorg Med Chem Lett. 2000 May 15;10(10):1117-20.

PubMed ID

10843231 [ View in PubMed

]

Abstract

Several aromatic/heterocyclic sulfonamides possessing free amino, imino or hydrazino moieties were transformed into the corresponding N-morpholylthiocarbonylsulfenyl derivatives, by reaction with N-morpholyldithiocarbamate in the presence of oxidizing agents (NaClO or iodine). These compounds showed nanomolar inhibition against three CA isozymes, and interesting in vitro tumor cell growth inhibitory properties, against several leukemia, non-small cell lung, ovarian, melanoma, colon, CNS, renal, prostate and breast cancer cell lines.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
4-(2-AMINOETHYL)BENZENESULFONAMIDE	Carbonic anhydrase 2	Ki (nM)	160	N/A	N/A	Details
Dorzolamide	Carbonic anhydrase 1	Ki (nM)	50000	N/A	N/A	Details
Dorzolamide	Carbonic anhydrase 2	Ki (nM)	9	N/A	N/A	Details