74131-06-9Relevant articles and documents
Nucleic acid probe, method for designing nucleic acid probe, and method for detecting target sequence
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Page/Page column 49, (2018/02/28)
The present invention provides a nucleic acid probe that can achieve high detection sensitivity and high specificity in mutation detection, mismatch detection, etc. by the PCR method, a method for designing such a nucleic acid probe, and a method for detecting a target sequence. The nucleic acid probe includes a nucleic acid molecule, and the nucleic acid molecule includes a plurality of fluorescent dye moieties that exhibit an excitonic effect. At least two of the fluorescent dye moieties that exhibit an excitonic effect are bound to the same base or two adjacent bases in the nucleic acid molecule with each fluorescent dye moiety being bound via a linker (a linking atom or a linking atomic group). The extension-side end of the nucleic acid molecule is chemically modified, thereby preventing an extension reaction of the nucleic acid molecule.
Pd-imidate complexes as recyclable catalysts for the synthesis of C5-alkenylated pyrimidine nucleosides via Heck cross-coupling reaction
Ardhapure, Ajaykumar V.,Sanghvi, Yogesh S.,Kapdi, Anant R.,García, Joaquín,Sanchez, Gregorio,Lozano, Pedro,Serrano, J. Luis
, p. 24558 - 24563 (2015/03/30)
Pd-imidate complexes have been employed as efficient catalysts for the Heck alkenylation of unprotected 5-iodo-2′-deoxyuridine in acetonitrile. The protocol was also shown to work well for the unprotected 5-iodo-2′-deoxycytidine. A highly efficient scale-up synthesis of the HSV-1 inhibitor Brivudine (BVDU) is also accomplished in an overall yield of 72% over 3-steps. The catalyst also showed recyclability for 3 consecutive runs.
Synthesis, cytotoxicity, and insight into the mode of action of Re(CO) 3 thymidine complexes
Bartholomae, Mark D.,Vortherms, Anthony R.,Hillier, Shawn,Ploier, Birgit,Joyal, John,Babich, John,Doyle, Robert P.,Zubieta, Jon
experimental part, p. 1513 - 1529 (2011/11/29)
Nucleoside analogues are extensively used in the treatment of cancer and viral diseases. The antiproliferative properties of organorhenium(I) complexes, however, have been scarcely explored to date. Herein we present the syntheses, characterization, and in vitro evaluation of ReI(CO)3 core complexes of thymidine and uridine. For the binding of the Re I(CO)3 core, a tridentate dipicolylamine metal chelate was introduced at positions C5′, C2′, N3, and C5 with spacers of various lengths. The corresponding organometallic thymidine complexes were fully characterized by IR and NMR spectroscopy and mass spectrometry. Their cytotoxicity was assessed against the A549 lung carcinoma cell line. Toxicity is dependent on the site and mode of conjugation as well as on the nature and the length of the tether. Moderate toxicity was observed for conjugates carrying the rhenium moiety at position C5′ or N3 (IC50=124-160 μm). No toxicity was observed for complexes modified at C2′ or C5. Complex 53, with a dodecylene spacer at C5′, exhibits remarkable toxicity and is more potent than cisplatin, with an IC50 value of 6.0 μm. To the best of our knowledge, this is the first report of the antiproliferative properties of [M(CO)3]+1-nucleoside conjugates. In competitive inhibition experiments with A549 cell lysates and purified recombinant human thymidine kinase 1 (hTK-1), enzyme inhibition was observed for complexes modified at either N3 or C5′, but our results suggest that the toxicity cannot be attributed solely to interaction with hTK-1.
