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Christian Krog-Jensen Mette K. Christensen Morten Meldal 《Letters in Peptide Science》1999,6(4):193-197
A new and facile synthesis of tyrosine phosphorylated peptides has been developed. N-Fmoc-TyrtBu)-OPfp was treated with TFA, phosphorylated with phosphorous oxychloride and the resulting phosphoric acid dichloride was hydrolysed to give N-Fmoc-Tyr(PO3H32)-OPfp 1 in an overall yield of 98%. Compound 1 was used in solid-phase peptide synthesis of phosphopeptides 2, 3 and 4, which are fragments of murine adipocyte lipid binding protein. The advantage of using the Pfp ester was the absence of pyrophosphates and other byproducts. 相似文献
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Uddin MK Reignier SG Coulter T Montalbetti C Grånäs C Butcher S Krog-Jensen C Felding J 《Bioorganic & medicinal chemistry letters》2007,17(10):2854-2857
Syntheses and structure-antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF(3), and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affecting the MDA-231 cell line. The best compounds from this series showed low nanomolar antiproliferative activity towards the MDA-468 cell line and a 1000-fold selectivity over the MDA-231 cell line. 相似文献
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Krog-Jensen Christian Christensen Mette K. Meldal Morten 《International journal of peptide research and therapeutics》1999,6(4):193-197
Summary A new and facile synthesis of tyrosine phosphorylated peptides has been developed.N
α-Fmoc-Tyr(tBu)-OPfp was treated with TFA, phosphorylated with phosphorous oxychloride and the resulting phosphoric acid dichloride was
hydrolysed to giveN
α-Fmoc-Tyr(PO3H2)-OPfp1 in an overall yield of 98%. Compound1 was used in solid-phase peptide synthesis of phosphopeptides2, 3 and4, which are fragments of murine adipocyte lipid binding protein. The advantage of using the Pfp ester was the absence of pyrophosphates
and other byproducts. 相似文献
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