Synthesis and cytotoxicity of novel 1-arylindolizines and 1-arylpyrrolo[2,1-a]isoquinolines

An efficient approach to the synthesis of indolizines and pyrrolo[2,1-a]isoquinolines based on a domino reaction is described. The reactivity of the derivatives and the structure-activity analysis are carried out in a number of the obtained compounds. We found a hit showing high cytotoxicity on tumor cells (IC50 = 5.92 ± 0.08 µM) whose cytotoxic effect is comparable to that of the known topoisomerase I inhibitor camptothecin. © 2021 Elsevier Ltd