title: Synthesis and cytotoxic activity of N-(2-pyridylsulfenyl)urea derivatives. A new class of potential antineoplastic agents.
abstract: Starting from a 3D-model for the antineoplastic activity of diarylsulfonylureas several new features were proposed and tested. Both types of assayed compounds, the N-(2-pyridylsulfonyl)urea and N-(2-pyridylsulfenyl)urea derivatives, inhibited by 50% the growth of the CCRF-CEM cell line at a dosage near to 1 microM. The N -(2-pyrimidinyl) derivative of the sulfenylurea 6c showed a better profile against HT-29, K-562 and HTB-54 tumor cell lines than the corresponding sulfonylurea 6b. Structural modifications on aryl systems affected differently to the cytotoxic activity shown by the compounds against each cell line.
authors.affiliation: Departamento de Química, Universidad Pública de Navarra, Pamplona, Spain.
authors.forename: M J
authors.initials: MJ
authors.lastname: Gil
authors.forename: M A
authors.initials: MA
authors.lastname: Mañú
authors.forename: C
authors.initials: C
authors.lastname: Arteaga
authors.forename: M
authors.initials: M
authors.lastname: Migliaccio
authors.forename: I
authors.initials: I
authors.lastname: Encío
authors.forename: A
authors.initials: A
authors.lastname: González
authors.forename: V
authors.initials: V
authors.lastname: Martínez-Merino
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry*; D014407:Tumor Cells, Cultured; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; C121725:N-((3-ethoxycarbonylpyridin-2-yl)thio)-N'-(2-pyrimidinyl)urea; D011743:Pyrimidines; D014508:Urea