The Experts below are selected from a list of 234 Experts worldwide ranked by ideXlab platform
Biliang Zhang - One of the best experts on this subject based on the ideXlab platform.
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Synthesis of 5'-deoxy-5'-thioguanosine-5'-monophosphorothioate and its incorporation into RNA 5'-termini.
Organic Letters, 2001Co-Authors: Biliang ZhangAbstract:5‘-Deoxy-5‘-thioguanosine-5‘-monophosphorothioate (GSMP) was synthesized in four steps with 35% overall yield. GSMP serves as a good substrate for in vitro transcription with T7 RNA polymerase to yield 5‘-GSMP-RNA, which was converted to 5‘-HS-RNA by dephosphorylation with alkaline phosphatase. The thiol-reactive agents can be efficiently introduced into the 5‘-terminus of RNA.
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Synthesis of 5'-deoxy-5'-thioguanosine-5'-monophosphorothioate and its incorporation into RNA 5'-termini.
Organic letters, 2001Co-Authors: Biliang Zhang, Zhiyong Cui, Lele SunAbstract:[figure: see text] 5'-Deoxy-5'-thioguanosine-5'-monophosphorothioate (GSMP) was synthesized in four steps with 35% overall yield. GSMP serves as a good substrate for in vitro transcription with T7 RNA polymerase to yield 5'-GSMP-RNA, which was converted to 5'-HS-RNA by dephosphorylation with alkaline phosphatase. The thiol-reactive agents can be efficiently introduced into the 5'-terminus of RNA.
Stewart W Schneller - One of the best experts on this subject based on the ideXlab platform.
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The 5'-nor aristeromycin analogues of 5'-deoxy-5'-methylthioadenosine and 5'-deoxy-5'-thiophenyladenosine.
Nucleosides Nucleotides & Nucleic Acids, 2014Co-Authors: Stewart W SchnellerAbstract:To extend the potential of 5′-noraristeromycin (and its enantiomer) as potential antiviral candidates, the enantiomers of the carbocyclic 5′-nor derivatives of 5′-methylthio-5′-deoxyadenosine and 5′-phenylthio-5′-deoxyadenosine have been synthesized and evaluated. None of the compounds showed meaningful antiviral activity.
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5'-Fluoro-5'-deoxyaristeromycin.
Bioorganic & Medicinal Chemistry Letters, 2007Co-Authors: Wei-kuan Li, Stewart W SchnellerAbstract:Abstract 5′-Fluoro-5′-deoxyaristeromycin ( 2 ) has been prepared via a Mitsunobu coupling of (1 S ,2 S ,3 R ,4 S )-2,3-(cyclopentylidenedioxy)-4-fluoromethylcyclopentan-1-ol with N 6 -bis-boc protected adenine. This procedure is adaptable to preparing a number of 5′-fluoro-5′-deoxycarbocyclic nucleoside analogs with diversity in the heterocyclic base. Antiviral analysis found promising activity for 2 toward measles but no other viruses. No cytotoxicity was observed for 2 .
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Enantiospecific synthesis of 5′,5′,5′-trifluoro-5′-deoxyneplanocin A
Tetrahedron Letters, 2005Co-Authors: Stewart W SchnellerAbstract:Abstract (−)-(1 S ,4 R )-4-Hydroxy-2-cyclopenten-1-yl acetate provided a convenient entry point for a 12-step chiral preparation of 5′,5′,5′-trifluoro-5′-deoxyneplanocin A.
Yasutsuna Sasaki - One of the best experts on this subject based on the ideXlab platform.
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rabeprazole intake does not affect systemic exposure to capecitabine and its metabolites 5 deoxy 5 fluorocytidine 5 deoxy 5 fluorouridine and 5 fluorouracil
Cancer Chemotherapy and Pharmacology, 2019Co-Authors: Masae Sekido, Kenichi Fujita, Yutaro Kubota, Hiroo Ishida, Takehiro Takahashi, Ryotaro Ohkuma, Takuya Tsunoda, Fumihiro Ishikawa, Motoko Shibanuma, Yasutsuna SasakiAbstract:Several retrospective studies have shown that the antitumor efficacy of capecitabine-containing chemotherapy decreases when co-administered with a proton pump inhibitor (PPI). Although a reduction in capecitabine absorption by PPIs was proposed as the underlying mechanism, the effects of PPIs on capecitabine pharmacokinetics remain unclear. We prospectively examined the effects of rabeprazole on the pharmacokinetics of capecitabine and its metabolites. We enrolled patients administered adjuvant capecitabine plus oxaliplatin (CapeOX) for postoperative colorectal cancer (CRC) patients and metastatic CRC patients receiving CapeOX with/without bevacizumab. Patients receiving a PPI before registration were allocated to the rabeprazole group, and the PPI was changed to rabeprazole (20 mg/day) at least 1 week before the initiation of capecitabine treatment. On day 1, oral capecitabine (1000 mg/m2) was administered 1 h after rabeprazole intake. Oxaliplatin (and bevacizumab) administration on day 1 was shifted to day 2 for pharmacokinetic analysis of the first capecitabine dose. Plasma concentrations of capecitabine, 5′-deoxy-5-fluorocytidine, 5′-deoxy-5-fluorouridine, and 5-fluorouracil were analyzed by high-performance liquid chromatography. Effects of rabeprazole on inhibition of cell proliferation by each capecitabine metabolite were examined with colon cancer cells (COLO205 and HCT116). Five and 9 patients enrolled between September 2017 and July 2018 were allocated to rabeprazole and control groups, respectively. No significant effects of rabeprazole on area under the plasma concentration–time curve divided by capecitabine dose for capecitabine and its three metabolites were observed. Rabeprazole did not affect the proliferation inhibition of colon cancer cells by the respective capecitabine metabolites. Rabeprazole does not affect capecitabine pharmacokinetics.
Jan Balzarini - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine, 5'-isocyano-2',5'-dideoxyuridine, 3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine.
Journal of Medicinal Chemistry, 1991Co-Authors: Johann Hiebl, E. Zbiral, Jan BalzariniAbstract:: The 5'-azidonucleosides 3 and 4 were obtained by treating thymidine and 2'-deoxyuridine with TPP/DEAD/HN3. The 3'-O-silylated 5'-azido-5'-deoxythymidine 5 and the corresponding 2'-deoxyuridine derivative 6 were transformed to the formamides (7 and 8, respectively) and dehydrated to the protected 5'-isocyano derivatives 9 and 10; deblocking gave 5'-isocyano-5'-deoxythymidine (11) and 5'-isocyano-2',5'-dideoxyuridine (12). 2,3'-Anhydro-5'-formamido derivatives of thymidine and 2'-deoxyuridine (19 and 20, respectively) were prepared by three different ways. In the most direct synthesis 3 and 4 were transformed to the 2,3'-anhydro-5'- azidonucleosides 17 and 18 by using TPP/DEAD; following the reaction with TPP/HCO2COCH3 gave 19 and 20. Nucleophilic opening reaction with LiN3 yielded the 3'-azido-5'-formylamino derivatives 21 and 22. Dehydration to 3'-azido-5'-isocyano-3',5'-dideoxythymidine (23) and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine (24) was achieved with tosyl chloride/pyridine. In contrast with 3'-azido-3'-deoxythymidine, compounds 11, 12, 23, and 24 were devoid of any marked inhibitory effect against DNA and RNA viruses including human immunodeficiency virus type I (HIV).
Lele Sun - One of the best experts on this subject based on the ideXlab platform.
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Synthesis of 5'-deoxy-5'-thioguanosine-5'-monophosphorothioate and its incorporation into RNA 5'-termini.
Organic letters, 2001Co-Authors: Biliang Zhang, Zhiyong Cui, Lele SunAbstract:[figure: see text] 5'-Deoxy-5'-thioguanosine-5'-monophosphorothioate (GSMP) was synthesized in four steps with 35% overall yield. GSMP serves as a good substrate for in vitro transcription with T7 RNA polymerase to yield 5'-GSMP-RNA, which was converted to 5'-HS-RNA by dephosphorylation with alkaline phosphatase. The thiol-reactive agents can be efficiently introduced into the 5'-terminus of RNA.
