Chemistry and Anti-tumor Activity of Sperabillin Polymers

  • 飛田 恒明
    Discovery Research Division Takeda Chemical Industries, Ltd.,
  • 坪谷 重利
    Discovery Research Division Takeda Chemical Industries, Ltd.,
  • 堀 晃
    Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
  • 村上 守生
    Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
  • 夏苅 英昭
    Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
  • 香西 義雄
    Pharmaceutical Research Division Takeda Chemical Industries, Ltd.,
  • 原田 節夫
    Discovery Research Division Takeda Chemical Industries, Ltd.,

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抄録

Sperabillin A, 3-[[(3R, 5R)-3-amino-6-[(2E, 4Z)-2,4-hexadienoylamino]-5-hydroxyhexanoyl]amino]propanamidine dihydrochloride, was polymerized on standing for several days under a highly humid atmosphere or in the presence of radical initiators. The average molecular weight of the polymers obtained could be regulated by changing the reaction conditions in the latter case. Spectral analyses of the polymers revealed that the 2,4-hexadienoyl moiety of sperabillins was polymerized in a free radical-initiated reaction. The polymers selectively inhibited the proliferation of human umbilical vein endothelial (HUVE) cells. Polymers having higher molecular weight showed stronger inhibition of HUVE cell proliferation. In addition, the polymers showed anti-tumor activity against B16 melanoma in vivo.

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詳細情報 詳細情報について

  • CRID
    1572261552254471296
  • NII論文ID
    110003630516
  • NII書誌ID
    AA00602100
  • ISSN
    00092363
  • 本文言語コード
    en
  • データソース種別
    • CiNii Articles

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