Cortistatin A をモチーフとする抗腫瘍活性リード化合物の創製

• 古徳 直之

  大阪大学大学院薬学研究科

書誌事項

タイトル別名

• Creation of Readily Accessible Analogue of Cortistatin A as an Antitumor Drug Lead
• Cortistatin A オ モチーフ ト スル コウシュヨウ カッセイ リード カゴウブツ ノ ソウセイ

抄録

  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 (1), 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 in vivo antiangiogenic activity and significant antitumor effect by oral administration.<br>

収録刊行物

• 薬学雑誌

  薬学雑誌 133 (8), 867-872, 2013-08-01

  公益社団法人 日本薬学会

キーワード

• cortistatin A
• antiangiogenesis
• marine sponge
• analogue synthesis
• structure-activity relationship

詳細情報

• CRID: 1390001206128910976
• NII論文ID: 130003361979
• NII書誌ID: AN00284903
• DOI: 10.1248/yakushi.13-00159
• COI: 1:STN:280:DC%2BC3sflsleitg%3D%3D
• ISSN: 13475231
• ISSN: 00316903
• NDL書誌ID: 024827558
• PubMed: 23903226
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I024827558
• Web Site: https://www.jstage.jst.go.jp/article/yakushi/133/8/133_13-00159/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2013371908
• 本文言語コード: ja
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
  • KAKEN
• 抄録ライセンスフラグ: 使用不可