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 doublestranded DNA in vitro and caused apoptosis of tumor cells including those that are resistant to several chemotherapeutic drugs.Porphyrins accumulate predominantly in tumor cells. This valuable feature makes natural and synthetic porphyrins attractive for conjugation with boron compounds and useful for boron neutron capture therapy of cancer (BNTC) 1,2 . Boronated porphyrins have been recently proposed to be employed for delivery of boron to tumors in BNTC and as photosensitizers in photodynamic therapy (PDT) 3,4 . Furthermore, boronated porphyrins can be visualized in cells and tissues by fluorescent microscopy. In the cells boronated porphyrins can interact with DNA due to their planar structure 5,6 . These characteristics together with physical treatments (thermal
The paper discusses the possible mechanisms of antitumor action of indolocarbazole derivatives. Here we present a data that show interaction drugs based on indolocarbazole derivatives with several intracellular targets and consequently activation different pathways of cell death. Also we present results of our studies on the mechanisms of antitumor action of compounds LCS-1006 and LCS-1208 synthesized in the N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia.
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