Synthesis of the first conjugates of 5-ethynyl-2′-deoxyuridine with closo-dodecaborate and cobalt-bis-dicarbollide boron clusters” Tetrahedronстатья
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Дата последнего поиска статьи во внешних источниках: 18 марта 2017 г.
Аннотация:A new 2'-deoxyuridine modification, 3',5'-bis-(dimethyl-t-butylsilyl)-5-(3-(2-(dimethylamino)ethoxy)-3-methylbutyn-1-yl)-2'-deoxyuridine was effectively synthesized in four easy steps. Its reactivity towards a range of cyclic oxonium adducts of closo-dodecaborate and cobalt-bis-dicarbollide boron clusters was studied. The cleavage reactions of cluster oxonium rings by the N,N-dimethylamino group of the modified nucleoside led to 5-ethynyl-2'-deoxyuridine conjugates with [B12H12]2- and [Co(C2B9H11)2]-, respectively. Cytotoxicity of these new conjugates in several cell lines was examined. Closo-dodecaborate conjugates showed low cytotoxicity in all examined cell lines, an advantageous and preferred property for potential boron delivering drugs for the boron neutron capture therapy (BNCT) of tumors.