Synthesis of new aromatic pyrrolo[2,1-c][1,4]benzodiazepines and pyrrolo[1,2-a]thieno[3,2-e][1,4]diazepines as anti-tumoral agents

Abstract

Diazepine analogs of thieno[2,3-b]pyrrolizin-8-ones were synthesized by aromatization of 2-hydroxypyrrolo[1,2-α]thieno[3,2-e][1,4]diazepines. These compounds were evaluated in vitro for their antiproliferative activity against the L1210 leukemia cell line. The activity of these compounds was in the micromolar range, the best result being for the mixture of the isomers 5 and 6 which showed a 0.35 μM IC50 against cell growth.