Synthesis and antitumor activity of novel cyclopropapyrroloindole (CPI) derivatives bearing bis(methoxycarbonyl) groups

Article abstract of DOI:10.1016/S0960-894X(97)00099-1

The title synthesis was achieved by employing oxidative cyclization of the enaminodiester prepared by Michael addition of the 5-aminoindoline with dimethyl acetylenedicarboxylate, as a key step. Some of these novel bis(methoxycarbonyl)cyclopropapynroloindole (MC₂CPI) derivatives 9c, d and their seco-chlorides 18c, d were found to exhibit prominent cytotoxicity and antitumor activity against P388 murine leukemia.