Discovering some novel tetrahydroquinoline derivatives bearing the biologically active sulfonamide moiety as a new class of antitumor agents

The present article describes the synthesis of some novel 4-(2-amino-3-cyano-4-(substituted-aryl)-5oxo-5,6,7,8-tetrahydroquinolin-1(4H)-yl)benzenesulfonamide (23-41) starting with 4-(3-oxo-cyclohex-1-enylamino)benzenesulfonamide (3). All the newly synthesized compounds were evaluated for their in vitro antitumor activity. Compounds 32, 25, 41, 35, 33, and 37 with IC50 values (2.5, 3, 5, 10, 12, and 12.5 mu g/mL) are more potent and efficacious than Doxorubicin (CAS-23214-92-8) as reference drug with (IC50 value = 37.5 mu g/mL). Also, compounds 28, 30, 31, and 34 (with IC50 values = 25 mu g/mL) are nearly as active as Doxorubicin. (C) 2010 Elsevier Masson SAS. All rights reserved.