Sixteen C-2-substituted quinolines were tested in both human cancer cell lines (MCF-7, H-460 and SF-268) and normal cell lines (Vero and THP-1). Preliminary results indicate that 2-α-furyl- and 2-γ-pyridinyl quinoline derivatives 1, 13 and 14 are active against three human cancer cell lines and, at the same time, were devoid of cytotoxic effect on normal cells. Biological activity and SAR results were compared with different molecular descriptors determined in silico using online available software, in an attempt to show a relationship with the possible mode of action of these quinoline derivatives. Keywords: C-2-aryl quinoline derivatives, Synthesis, Anticancer activity, Cytotoxicity on normal cells, Toxic effects in silico, MCF-7, cytotoxic effect, Biological activity, SAR results, pathological proliferation , cisplatin, adriamycin, doxorubicin, anthracycline, antibiotic