Synthesis and in vitro antiproliferative effect of novel quinoline-based potential anticancer agents

Several derivatives with a quinoline scaffold and a flexible, semi-flexible or rigid side chains at position 8 of the quinoline ring were synthesized and assessed for their in vitro activity versus the human colon cancer cell line HT29 and the human breast cancer cell line MDA-MB231. The HT29 cell line was more refractory to the cytotoxic activity of some compounds, meanwhile all the quinoline derivatives except one displayed high to moderate activity against MDA-MB231 with IC50 values ranging between 4.6 and 48.2 μM. The most active derivative in this study against both tested cell lines was the Schiff's base 4e with IC50 of 4.7 and 4.6 μM against HT29 and MDA-MB231, respectively.

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► 15 New 8-substituted quinolines with flexible, semi-flexible or rigid side chains.
► Antiproliferative screening against HT29 and MDA-MB231 human cancer cell lines.
► Analogs with a rigid side chain were more active against HT29.
► MDA-MB231 cell line was more responsive to flexible or semi-flexible analogs.