Boronated conjugates of protohemin IX with L-amino acids: Synthesis and antitumor activity

Abstract

We report the synthesis of novel conjugates of protohemin IX with neutral and anionic boron polyhedra and L-amino acids. The amino acids are linked to the porphyrin macrocycle via the amide or ester bond. The serine containing boronated protohemin was the most cytotoxic for K562 human leukemia cell line. This compound interacted with double-stranded DNA in vitro and caused apoptosis of tumor cells including those that are resistant to several chemotherapeutic drugs.