title: 4-toluenesulfonylureido derivatives of amines, amino acids and dipeptides: a novel class of potential antitumor agents.
abstract: The screening of a series of arylsulfonylureido derivatives of amines (such as histamine, or dopamine), aliphatic/aromatic amino acids (such as Gly, beta-Ala, Val, Lys, Arg, Phe, Tyr, DOPA, etc.) and dipeptides (such as GlyGly, beta-AlaHis) led to the identification of three derivatives that possess tumor growth inhibitory properties against several leukemia, non-small cell lung, ovarian, melanoma, colon, CNS, renal, and breast cancer cell lines in vitro. The new derivatives were prepared by reaction of 4-toluenesulfonyl isocyanate with (protected) amines, amino acids or dipeptides. The mechanism of antitumor action with these new derivatives is not known at the moment but it may imply uncoupling of mitochondria, as for the structurally related diarylsulfonylurea sulofenur, an investigational anticancer agent.
authors.affiliation: Università degli Studi, Dipartimento di Scienze Dermatologiche, Centro MTS, Via degli Alfani 37, 50122, Firenze, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Mastrolorenzo
authors.forename: A
authors.initials: A
authors.lastname: Scozzafava
authors.forename: C T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D000588:Amines / Q000737:chemistry*; D000596:Amino Acids / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry*; D004151:Dipeptides / Q000737:chemistry*; D014105:Tosyl Compounds / Q000737:chemistry*; D014407:Tumor Cells, Cultured
chemical_list: D000588:Amines; D000596:Amino Acids; D000970:Antineoplastic Agents; D004151:Dipeptides; D014105:Tosyl Compounds