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

Starting from a 3D-model for the antineoplastic activity of diarylsulfonylu reas several new features were proposed and tested. Both types of assayed c ompounds, the N-(2-pyridylsulfonyl)urea and N-(2-pyridylsulfenyl)urea deriv atives, inhibited by 50% the growth of the CCRF-CEM cell line at a dosage n ear to 1 mu M The N-(2-pyrimidinyl) derivative of the sulfenylurea 6c showe d a better profile against HT-29, K-562 and HTB-54 tumor cell lines than th e corresponding sulfonylurea 6b. Structural modifications on aryl systems a ffected differently to the cytotoxic activity shown by the compounds agains t each cell line. (C) 1999 Elsevier Science Ltd. All rights reserved.