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

• DOI: 10.1016/j.tetlet.2021.153552
• Publication Date: 2021-11-19T21:42:32Z
• Authors: Alisa A. Nevskaya; Almira R. Miftyak...; Lada V. Anikina; Tatiana N. Borisova; Aleksey V. Varlamov; Leonid G. Voskres...
• Keywords: Isoquinoline

Abstract 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.