99 中性子捕捉療法による癌治療のためのホウ素キャリアーの設計と合成(ポスター発表の部)

概要

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Several new methods for the synthesis of boron-10 carriers have been developed for boron neutron capture therapy (BNCT). Two new methods for the synthesis of nucleosides having arylboronic moiety have been developed (Scheme 1 and 2). Chemistry of o-carborane has been studied since it is a nice candidate for BNCT in order to deliver sufficient quantity of boron atoms to tumor cells. The carbon-carbon bond formation reaction to o-carboranes proceeding under essentially neutral conditions has been accomplished for the first time (Scheme 3). o-Carboranes having a cascade type of polyglycerols 5 have been synthesized since o-carborane itself has strong lipophilic nature which causes a serious problem for the design of its derivatives (Scheme 4). The water solubility of 6 and 7 is 0.67M and 5.44M, respectively. Nucleoside derivatives having o-carborane moiety have been synthesized via palladium catalyzed coupling reaction and o-carborane formation reaction with decaborane-14 (Scheme 5). The biological activity of 11a, and 11b have been examined in vitro using B16 melanoma cells and TIG-I-20 Fibroblast cells. The boron atom is selectively concentrated in B16 Melanoma cells (model of a cancer cell), compared with in Hybroblast cells (model of a normal cell).
天然有機化合物討論会の論文
1992-09-10