Cortistatin A をモチーフとする抗腫瘍活性リード化合物の創製  [in Japanese] Creation of Readily Accessible Analogue of Cortistatin A as an Antitumor Drug Lead  [in Japanese]

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Author(s)

Abstract

  Angiogenesis, the formation of new blood capillaries from preexisting blood vessels, is a vital process in growth of solid tumors and development to malignant stage. This makes angiogenesis a desirable target for cancer treatment. In this work, design and syntheses of structurally simplified analogues of cortistatin A (<b>1</b>), a novel antiangiogenic steroidal alkaloid from Indonesian marine sponge, and their biological activities were investigated. One of the analogues, in which the isoquinoline moiety was appended to the planar tetracyclic core structure, showed potent antiproliferative activity against human umbilical vein endothelial cells (HUVECs) together with high selectivity and also showed <i>in vivo</i> antiangiogenic activity and significant antitumor effect by oral administration.<br>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 133(8), 867-872, 2013

    The Pharmaceutical Society of Japan

Codes

  • NII Article ID (NAID)
    130003361979
  • NII NACSIS-CAT ID (NCID)
    AN00284903
  • Text Lang
    JPN
  • ISSN
    0031-6903
  • NDL Article ID
    024827558
  • NDL Call No.
    Z19-411
  • Data Source
    NDL  J-STAGE 
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