Synthesis and Antitumor Activity of Glycoside Drivatives Containing Posphonate
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Project supported by the Technology Department of Guizhou Province (No. G[2014]7013)

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    Abstract:

    A series of title compounds(Ⅲa-Ⅲf) were synthesized via microwave-assisted by the yield of 79.6%-84.1%, with α-hydroxyphosphonate and bromo mono-saccharide intermediates as raw materials, alkaline ionic liquid [Bmim]OH as catalyst. Their structures were confirmed by IR, 1HNMR and 13CNMR, and their antiproliferative activities were evaluated in some tumor cell lines by MTT assay. Prelimi-nary results in bioactivity tests indicated that some title compounds exhibited better activity. Among them, compounds Ⅲa, Ⅲb containing the glucose group had better inhibition effect against SGC-7901 with IC50 values of 12.9 ± 0.9μmol/L, 14.3± 1.1μmol/L respectively, compounds Ⅲc, Ⅲd containing the galactose fragments showed remarkable activities against A-549 with IC50 values of 15.9 ± 0.9μmol/L and 14.2 ± 1.3 μmol/L respectively.

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History
  • Received:April 09,2018
  • Revised:June 11,2018
  • Adopted:June 14,2018
  • Online: November 08,2018
  • Published:
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