Robins, Morris J. published the artcileImproved Syntheses of 5′-S-(2-Aminoethyl)-6-N-(4-nitrobenzyl)-5′-thioadenosine (SAENTA), Analogues, and Fluorescent Probe Conjugates: Analysis of Cell-Surface Human Equilibrative Nucleoside Transporter 1 (hENT1) Levels for Prediction of the Antitumor Efficacy of Gemcitabine, Quality Control of 1869-45-0, the publication is Journal of Medicinal Chemistry (2010), 53(16), 6040-6053, database is CAplus and MEDLINE.
5′-S-(2-Aminoethyl)-6-N-(4-nitrobenzyl)-5′-thioadenosine (SAENTA), 5′-S-(2-acetamidoethyl)-6-N-[(4-substituted)benzyl]-5′-thioadenosine analogs, 5′-S-[2-(6-aminohexanamido)]ethyl-6-N-(4-nitrobenzyl)-5′-thioadenosine (SAHENTA), and related compounds were synthesized by SNAr displacement of fluoride from 6-fluoropurine intermediates with 4-(substituted)-benzylamines. Conjugation of the pendant amino groups of SAENTA and SAHENTA with fluorescein-5-yl isothiocyanate (FITC) gave fluorescent probes that bound at nanomolar concentrations specifically to human equilibrative nucleoside transporter 1 (hENT1) produced in recombinant form in model expression systems and in native form in cancer cell lines. Transporter binding effects were studied and the ability of the probes to predict the potential antitumor efficacy of 2′-deoxy-2′,2′-difluorocytidine (gemcitabine) was demonstrated.
Journal of Medicinal Chemistry published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, Quality Control of 1869-45-0.
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