Evaluation of in vitro cytotoxicity of carboranyl amino acids, their chemical precursors and nido carboranyl amino acids for boron neutron capture therapy.

摘要: The purpose of the present study was to define in vitro cellular toxicity three carborane-containing amino acids: p-(o-carboran-yl)-phenylalanine (CBPA), O-(o-carboran-1-ylmethyl)-tyrosine (CBT), and o-carboranylalanine (CBA), which are analogues phenylalanine, tyrosine, alanine respectively. In addition, two their chemical precursors: CBACN (B10H11C2-CH2CHNH2CN) CBTCN (B10H11C2-CH2OC6H4CH2CHNH2CN) nido CBA were evaluated for on human MRA 27 melanoma cells. Hydroxypropyl-beta-cyclodextrin (beta-CD) initially used solubilize all compounds except assays Cells incubated with test at varying concentrations 24 hrs, following proliferative activity surviving cells determined by pulsing tritiated thymidine ([3H]-TdR) an additional 18 hrs. CBT a concentration 280 micrograms/ml non-toxic when solubilized beta-CD. 350 beta-CD, but DMSO produced 50% reduction uptake [3H]-TdR 75 micrograms/ml. CBPA, nontoxic 400 micrograms/ml, while 50 40 respectively, both toxic, even Nido medium non-toxic. Although these boron precludes use as capture agents Neutron Capture Therapy, they may have some potential cytoreductive chemotherapy cancer, further evaluation be warranted.