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Alpha (α-) and beta (β-carboranyl-C-deoxyribosides: syntheses, structures and biological evaluation.

Abstract：

:The syntheses of the unprotected neutral closo-carboranyl-C-deoxyriboses, starting from anomeric mixture of 1-ethynyldeoxyriboses, and their corresponding open-cage nido-derivatives have been described. The structures of both the α- and β-anomers were confirmed by single-crystal X-ray diffraction. While limited water solubility of the neutral closo-anomers led to high cytotoxicity, their cesium salts (nido-species) exhibited higher water solubility leading to lower cytotoxicity. However, in vitro boron neutron capture therapy (BNCT) investigation using the murine squamous cell carcinoma (SCCVII) cell lines showed that there are no significant differences between the survival fractions of the two species.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Šnajdr I,Janoušek Z,Takagaki M,Císařová I,Hosmane NS,Kotora M

doi

10.1016/j.ejmech.2014.06.005

subject

Has Abstract

pub_date

2014-08-18 00:00:00

pages

389-97

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00523-6

journal_volume

83

pub_type

杂志文章

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