In vitro and in vivo activities of a small series of α-bromoacrylic derivatives of low molecular weight (MW) are described and compared with those of α-bromoacrylic derivatives of distamycin-like frames. Low MW compounds, when lacking of a strong basic moiety, are potent cytotoxics, while analogues bearing a strong basic moiety are not. This suggests the existence of an active transport mechanism for distamycin-derived cytotoxics ...