Both benzimidazole and quinoline are found in various biologically active compounds [1, 2]. As a part of our ongoing efforts [3, 4] to prepare novel 7-chloro-4-aminoquinoline hybrid compounds, herein we present synthesis of 23 novel quinoline- benzimidazoles which were evaluated on one non- tumor (MRC-5) and 5 tumor cell lines (HeLa, CaCo- 2, HL-60, THP-1, and HuT78). Results revealed that non-amidine compounds have strong, albeit not selective, antiproliferative activity against all the cell lines, with GI50 ranging from 1 to 10 μM. Cyclopentyl-amidine derivatives, have shown to be more selective with moderate to strong activity against leukemia and lymphoma tumor cell lines.