Synthesis of some sulfonamides, disubstituted sulfonylureas or thioureas and some structurally related variants. A class of promising antitumor agents

摘要: Some new benzenesulfonamides, disubstituted sulfonylureas, and sulfonylthioureas substituted basically with 3-(2-thienyl or 3-pyridyl)-indeno[1,2-c]pyrazol(in)e counterpart were synthesized to be evaluated for their in vitro antitumor activity. of the thioureido derivatives cyclized corresponding five-membered thiazolidinons, thiazolines, six-membered thiazinones as interesting structure variants. According protocol National Cancer Institute (NCI) disease-oriented human cells screening panel assay, 13 compounds showed promising broad spectrum In general, containing thienyl moiety displayed better spectra than those pyridyl moiety. Compound 5, 4-(3-(2-thienyl)-3H-indeno[1,2-c]pyrazol-2-yl)-benzenesulfonamide [GI50, TGI, LC50 (MG-MID) values 13.2, 33.1 69.2 μM, respectively] proved most active member this study variable degrees potencies against all tested subpanel tumor cell lines particular effectiveness leukemia prostate subpanels at both GI50 (3.30 8.68 μM, respectively) TGI levels (15.7 22.3 μM, respectively).