, Volume 16, Issue 6, pp 300-318
Date: 30 Oct 2007

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

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