Designed as potential cytotoxic agents a series of 6-substituted 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinoline derivatives were synthesized by using a Bischler type reaction. The methodology involved the cyclodehydration of 2-(3,4-dihydroquinolin-1(2H)-yl)-1-alkyl/aryl ethanones in the presence of p-TSA under ultrasound irradiation. A number of compounds were prepared using this methodology and tested for their in vitro anti-proliferative properties against cancer (leukemia) and non-cancerous cell lines. Some of the compounds showed promising and selective cytotoxic effects toward leukemia cells. ª 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).