Cytotoxic alpha-bromoacrylic derivatives of low molecular weight

…, M Caldarelli, C Geroni, N Mongelli, B Reinach…

Index: Beria, Italo; Caldarelli, Marina; Geroni, Cristina; Mongelli, Nicola; Reinach, Benedetta; Vignati, Luisella; Cozzi, Paolo Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 11 p. 1467 - 1471

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Citation Number: 5

Abstract

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 ...