Synthesis, Tissue Uptake, and Toxicity of a Nickel Tetracarboranylphenylporphyrin
Porphyrins have been used for boron neutron capture therapy [BNCT] and photodynamic therapy [PDT] of experimental rodent tumors. PDT requires much less porphyrin than BNCT, typically 5 μg as compared to > 200 μg per gram body weight [gbw]. Toxicity is a major consideration in the use of boronated drugs for BNCT. At 265 μg/gbw, a boronated porphyrin, VCDP  (Figure 1) delivered 40 μg B/g to tumor tissue 4 days after the last of 12 intraperitoneal [ip] injections.1 There was transient hematologic and hepatic toxicity. If the VCDP dose rate was kept low (22 μg/gbw per ip injection; 12 injections over 4 days), lethality was under 10%. A tetraphenylporphyrin  containing four meta-nido-carborane cages was synthesized2 and when tested in mice found to be much more toxic than VCDP.
KeywordsBoron Concentration Boron Neutron Capture Therapy Diacetic Acid Boron Analysis Carborane Cage
Unable to display preview. Download preview PDF.
- 5.G.P. Chiusoli, M. Costa, S. Reverberi, Synthesis of pyrrole-3,4-diacetic acid and its derivatives, Syn. 1989: 262–265.Google Scholar
- 9.M.M. Zuk, B.D. Rihter, M.E. Kenney, M.A.J. Rodgers and M. Kreimer-Birnbaum, Pharmacokinetic and tissue distribution studies of the photosensitizer bis(di-isobutyl octadecylsiloxy)silicon 2,3-naphthalocyanine (isoBOSINC) in normal and tumor-bearing rats, Photochem. Photobiol., 59: 66–72, 1994.PubMedCrossRefGoogle Scholar