Synthesis and biological evaluation of diarylamines with antitumor activity

By structural modifications of our previous leads 1−3, 18 diarylamines were designed, synthesized and evaluated with a human tumor cell line panel, including A549, DU145, KB, and KB-vin cell lines, resulting  in the discovery of new antitumor agents A6 and B2 with low micromolar GI₅₀ values ranging from 1.55−2.10 μmol·L⁻¹ for above cell lines, and A9 with GI₅₀ values ranging from 1.55−2.10 μmol·L⁻¹ specially for DU145, KB, and KB-vin cells.  Current structure-activity relationships are helpful for further lead optimization.