Studies on the synthesis of potent antitumor hybrids of the spliceosome inhibitors FR901464 and pladienolide

• Project/Area Number: 22590022
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Chemical pharmacy
• Research Institution: Hoshi University
• Principal Investigator: TSUBUKI Masayoshi 星薬科大学, 薬学部, 教授 (90163865)
• Project Period (FY): 2010 – 2012
• Project Status: Completed (Fiscal Year 2012)
• Budget Amount: ¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000); Fiscal Year 2012: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000); Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000); Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
• Keywords: 合成化学 / スプライシング阻害剤 / FR901464 / pladienolide / ハイブリッド誘導体 / SF3b / Dladienolide

Research Abstract

Since FR901464 and pladienolide have a very similar mechanism that would be the inhibition of SF3b, we developed a hypothetical hybrid that could have similar biological activity. We have succeeded in the synthesis of each parts of FR901464 and pladienolide.

Research Products

• [Journal Article] Synthesis and Evaluation of 4-Aryl-2(1H)-quinolinones as Potent Amyloid ss Fibrillogenesis Inhibitors (2012)
  • Author(s): Y. Shimokawa, M. Nakakoshi, S. Saitoh, H. Suzuki, Y. Yokoyama, A. Ishigami, H. Nishioka, and M. Tsubuki
  • Journal Title: Heterocycles Volume: Vol. 85 Pages: 1933-1940
  • Peer Reviewed
• [Journal Article] Synthesis and Evaluation of 4-Aryl-2(1H)-quinolinones as Potent Amyloid β Fibrillogenesis Inhibitors (2012)
  • Author(s): Yoko Shimokawa
  • Journal Title: Heterocycles Volume: 85 Issue: 8 Pages: 1933-1940
  • DOI: 10.3987/com-12-12506
  • Peer Reviewed
• [Journal Article] New Type of Matrix for Analysis of Low Molecular Weight Compounds by MALDI-TOF MS (2012)
  • Author(s): 中越雅道
  • Journal Title: Heterocycles Volume: 85 Issue: 4 Pages: 927-932
  • DOI: 10.3987/com-12-12438
  • Peer Reviewed
• [Journal Article] タンパク質翻訳阻害作用機構に基づく新規ながん治療薬の創製 (2011)
  • Author(s): 津吹政可
  • Journal Title: 星薬科大学紀要 Volume: Vol.53 Pages: 1-7
  • NAID: 40019183964
  • Peer Reviewed
• [Journal Article] Proteomic Analysis of Two Types of Exosomes in Human Whole Saliva (2011)
  • Author(s): 小川裕子
  • Journal Title: Biol.Pharm.Bull. Volume: 34 Pages: 13-23
  • Peer Reviewed
• [Journal Article] Enantioselective Synthesis of the C(2)-C(11) Cyclopropylfuran Segment of Pinnatin J (2010)
  • Author(s): M. Tsubuki, T. Abekura, K. Takahashi, and T. Honda
  • Journal Title: Heterocycles Volume: Vol.82 Pages: 319-323
  • Peer Reviewed
• [Presentation] スプライシング因子阻害活性を有するプラジエノリド及び FR901464 の合成研究 Part 1 (2012)
  • Author(s): 横江弘雅、 武井友香里、 松村茉莉、津吹政可
  • Organizer: オープン・リサーチ・センター整備事業研究報告会
  • Place of Presentation: 星薬科大学
  • Year and Date: 2012-02-23
• [Presentation] スプライシング因子阻害活性を有するプラジエノリド及びFR901464の合成研究Part2 (2012)
  • Author(s): 岡野恵里、齊藤友加里、津吹政可
  • Organizer: オープン・リサーチ・センター整備事業研究報告会
  • Place of Presentation: 星薬科大学
  • Year and Date: 2012-02-23
• [Presentation] スプライシング因子阻害作用を有するプラジエノリド及びFR901464の合成研究 (2011)
  • Author(s): 岡野恵里、齊藤友加里、武井友香里、松村茉莉、津吹政可
  • Organizer: 第55回日本薬学会関東支部大会
  • Place of Presentation: 千葉
  • Year and Date: 2011-10-08
• [Remarks]
  • URL: http://polaris.hoshi.ac.jp/kyoshitsu/seitaiyuki/index.html
• [Remarks] 星薬科大学生体分子有機学研究室ホームページ
  • URL: http://polaris.hoshi.ac.jp/kyoshitsu/seitaiyuki/index.html