Synthesis and antitumor activity of new benzoheterocyclic derivatives of distamycin A.

摘要: The design, synthesis, and in vivo vitro antileukemic activity of a novel series compounds (13−22 34), which different benzoheterocyclic rings, bearing nitrogen mustard or benzoyl an α-bromoacryloyl group as alkylating moieties, are tethered to distamycin frame, reported, structure−activity relationships discussed. new derivatives were prepared by coupling mustard-substituted, α-bromoacryloyl-substituted carboxylic acids 23−32 with desformyldistamycin (33) one case its two-pyrrole analogue 35. With very few exceptions, the activities same moiety slightly affected kind heteroatom present on ring. All compounds, exception, showed against L1210 murine leukemia cell line comparable better than that tallimustine. an...