Synthesis of Carborane-Containing Porphyrin Derivatives for the Boron Neutron Capture Therapy of Tumors

摘要: The treatment of malignant brain tumors using conventional therapies and surgery often leads to tumor recurrence and/or unwanted side effects. Boron neutroncapturetherapy(BNCT)isabinaryandlocalizedformoftreatmentforbrain other difficult-to-treat cancers that uses nontoxic boron-containing agents. Boronated porphyrins derivatives constitute a class highly promising third-generation boron delivery agents for BNCT. These stable, tumor-specific, fluorescent macrocycles can be synthesized with high content, deliver therapeuticamountsofborontotargetsites,andallowtumordetectionandtreatment planning by optical imaging. In addition, boronated have shown low toxicityandenhancedtumorselectivityandretentiontimescomparedwithclinically approved BNCT agents, BSH BPA. this article the synthesis carboranyl- containing application in is reviewed, special emphasis on reported last decade. Current strategies enhancing biological efficacy involve their association tumor-targeting molecules, such as polyamines peptides, improved selectivity accumulation.