Drug Discovery Today ( IF 7.4 ) Pub Date : 2017-09-05 , DOI: 10.1016/j.drudis.2017.08.009 Gianpiero Calabrese , Anis Daou , Eugen Barbu , John Tsibouklis
Boron neutron capture therapy (BNCT) is a promising targeted chemoradiotherapeutic technique for the management of invasive brain tumors, such as glioblastoma multiforme (GBM). A prerequisite for effective BNCT is the selective targeting of tumour cells with 10B-rich therapeutic moieties. To this end, polyhedral boranes, especially carboranes, have received considerable attention because they combine a high boron content with relative low toxicity and metabolic inertness. Here, we review progress in the molecular design of recently investigated carborane derivatives in light of the widely accepted performance requirements for effective BNCT.
中文翻译:
迈向碳硼烷官能化结构治疗脑癌
硼中子捕获疗法(BNCT)是一种有前途的靶向化学放射治疗技术,可用于治疗侵袭性脑肿瘤,例如多形性胶质母细胞瘤(GBM)。有效BNCT的先决条件是具有10个富含B的治疗部分对肿瘤细胞的选择性靶向。为此,多面体硼烷,尤其是碳硼烷,受到了广泛的关注,因为它们结合了高硼含量和相对较低的毒性和代谢惰性。在这里,我们根据有效的BNCT的广泛接受的性能要求,回顾最近研究的碳硼烷衍生物的分子设计进展。