期刊
APPLIED RADIATION AND ISOTOPES
卷 106, 期 -, 页码 251-255出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.apradiso.2015.06.031
关键词
Carboranyl thymidine analogs; N5-2OH; F98 rat glioma; BNCT
类别
资金
- NCI NIH HHS [5R01CA127935, R01 CA127935] Funding Source: Medline
In this report we describe studies with N5-2OH, a carboranyl thymidine analog (CTA), which is a substrate for thymidine kinase 1 (TK1), using the F98 rat glioma model. In vivo BNCT studies have demonstrated that intracerebral (i.c.) osmotic pump infusion of N5-2OH yielded survival data equivalent to those obtained with i.v. administration of boronophenylalanine (BPA). The combination of N5-2OH and BPA resulted in a modest increase in MST of F98 glioma bearing rats compared to a statistically significant increase with the RG2 glioma model, as has been previously reported by us (Barth et al., 2008). This had lead us to synthesize a second generation of CTAs that have improved in vitro enzyme kinetics and in vivo tumor uptake (Agarwal et al., 2015). (C) 2015 Elsevier Ltd. All rights reserved.
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