Materials, Methods & Technologies, Volume 11, 2017

Abstract: Physical methods in antitumor treatment are frequently used in combination (simultaneous or sequential) to achieve maximal effect. Therefore, the compound capable of sensitizing tumor cells to different types of energy (light, ionizing X-rays, thermal neutrons) would be applicable in more than one therapeutic modality. We synthesized a novel fluorinated boron-containing chlorin derivative {5,10,15,20-tetrakis[4-(1-carba-closo-dodecaboran-1-yl)tetrafluorophenyl]-17,18-dihydroporphyrin)] tetrasodium (Compound-B). In this compound the boron atoms are represented by boron-10. Compound-B showed a good water solubility and cytoplasmic accumulation, as well as low-to null dark cytotoxicity. Compound-B potently (at low M concentrations) sensitized the transplanted C6 glial tumor cells (a BALB-c-nu/nu murine model) to PDT and BNCT. Importantly, Compound-B also increased the efficacy of proton or carbon therapy. These results provide evidence that structural optimizations of known chemical classes may confer valuable characteristics to compounds initially designated for one particular therapeutic modality.