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Synthesis and cytotoxic activity of N-(2-pyridylsulfenyl)urea derivatives. A new class of potential antineoplastic agents

16-ago-1999 | Revista: Bioorganic and Medicinal Chemistry Letters

Gil MJ, Mañú MA, Arteaga C, Migliaccio M, Encío I, González A, Martínez-Merino V.

Departamento de Química, Universidad Pública de Navarra, Pamplona, Spain.


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.

CITA DEL ARTÍCULO  Bioorg Med Chem Lett. 1999 Aug 16;9(16):2321-4

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