An expeditious synthesis of cytotoxic pyrroloisoquinoline derivatives. Structure-activity comparative studies with isomeric pyrroloquinolines.

A number of pyrroloisoquinolines have been prepared by reaction of 5-nitroisoquinoline with vinylmagnesium bromide followed by N-alkylation with the appropriate 2-chloro-N,N-dialkylethylamine. Their cytotoxicity was evaluated in a number of ovarian cell lines and compared to their analogous isomeric pyrroloquinolines. Two of the new compounds, 7c and 7d, are selective toward the A2780 cisplatin-resistant line.