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.
Vlachou
Margarita
M
Department of Pharmaceutical Chemistry, School of Pharmacy, University of Athens, Panepistimiopolis-Zografou, 157-71 Athens, Greece.
Tsotinis
Andrew
A
Kelland
Lloyd R
LR
Thurston
David E
DE
D005260:Female; D006801:Humans; D007536:Isomerism; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000502:physiology
D007546:Isoquinolines; D011758:Pyrroles; C039109:isoquinoline