P-Carboranylalanine Analogs of BPA for NCT
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AbstractBoron Neutron Capture Therapy (BNCT) is a very promising therapy for certain tumors, such as gliomamelanomas. p-Boronophenylalanine (BPA), an analog of phenylalanine, is one of the leading BNCT agentundergoing clinical trials in the U.S. for the treatment of gliomas and melanomas. It has already beJapan for the treatment of melanoma. Although very effective, a major drawback of BPA is the high dorequired to achieve clinically effective concentration of boron- 10 in the tumor. It would be quitenew BPA analogs that retain the physico-chemical and bio-distribution properties of BPA, yet have hiThe Phase I studies are therefore designed to synthesize analogs of BPA with high boron content andfunctional groups. The high boron content will allow the use of smaller quantities of BNCT agents, wfunctional group provides a handle to control the physico-chemical properties to optimize the strucuptake and selectivity. The phase I studies will also evaluate the in vitro cell uptake and biologicPhase II research will focus on further structure optimization and in vivo BNCT efficacy and toxicol
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