Abstract
A bis(chloroethyl)amine-containing side chain is attached to an oxonaphthalene-annelated pyrrole in expectation of DNA alkylating properties. The cytotoxicity is evaluated against two cell lines, KB-31 and KB-8511, respectively.
Highlights
Nitrogen mustards were the first clinically effective cancer therapeutic agents
After stirring for 2 h at room temperature, the reaction mixture was concentrated under vacuum and the residue was dissolved in ethyl acetate
(b) The resulting crude product was purified by column chromatography to afford a solid residue which was dissolved in 25 mL of EtOH/H2O (3/1). 0.55 mL (0.61 g, 1.40 mmol) of oxirane were added to the reaction mixture at 0 °C
Summary
Nitrogen mustards were the first clinically effective cancer therapeutic agents. The cytotoxic effects are based on the highly active aziridinium cation intermediates arising from the bis(2-chloroethyl)amine moiety [1]. In continuation of our department’s previous studies in the field of antitumor agents [2,3,4,5,6,7,8,9], we are reporting in this paper the synthesis of the oxonaphthalene-annelated pyrrole 3 with an attached side chain containing a bis(2-chloroethyl)amine group. The cytotoxic activity of 3 was evaluated.
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