Synthesis of novel inhibitors of hypoxia-inducible factor-1 transcriptional pathway based on natural products

• Project/Area Number: 22710223
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Living organism molecular science
• Research Institution: Yokohama City University (2011); Keio University (2010)
• Principal Investigator: ISHIKAWA Yuichi 横浜市立大学, 国際総合科学部, 助教 (40348826)
• Project Period (FY): 2010 – 2011
• Project Status: Completed (Fiscal Year 2011)
• Budget Amount: ¥3,250,000 (Direct Cost: ¥2,500,000、Indirect Cost: ¥750,000); Fiscal Year 2011: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000); Fiscal Year 2010: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
• Keywords: 構造活性相関 / 低酸素 / ステロイド / 抗がん剤

Research Abstract

Synthesis of strongylophorine analogues, inhibitors of hypoxia-inducible factor-1(HIF-1) transcriptional pathway, was attempted. Considering the structure of strongylophorines, synthesis of analogue possessing a distinctive lactone structure commenced with cholesterol, easily available steroid compound. The efforts of functionalization against cholesterol derivatives provided the desired analogue.

Research Products

• [Journal Article] Design and synthesis of biotinylated DHMEQ for direct identification of its target NF-kB components (2011)
  • Author(s): Saitoh, T.; Takeiri, M.; Gotoh, Y.; Ishikawa, Y.; Umezawa, K.; Nishiyama, S.
  • Journal Title: Bioorganic & MedicinalChemistry Letters Volume: 21 Issue: 21 Pages: 6293-6296
  • DOI: 10.1016/j.bmcl.2011.08.122
  • Peer Reviewed
• [Journal Article] Synthesis of the C7-26 Fragment of Amphidinolides G and H (2011)
  • Author(s): Hara, A.; Morimoto, R.; Ishikawa, Y.; Nishiyama, S.
  • Journal Title: Organic Letters Volume: 13 Issue: 15 Pages: 4036-4039
  • DOI: 10.1021/ol201547q
  • Peer Reviewed
• [Journal Article] Does pretreatment with proton pump inhibitors influence the eradication rate of Helicobacter pylori? (2010)
  • Author(s): Tokoro C, Inamori M, Koide T, Iida H, Sakamoto Y, Endo H, Hosono K, Takahashi H, Yoneda M, Yasuzaki H, Ogawa M, Abe Y, Kubota K, Saitou S, Kawana I, Matsuda R, Takahashi D, Nakajima A.
  • Journal Title: Hepatogastroenterology Volume: 57 Issue: 1 Pages: 1645-9
  • DOI: 10.1016/j.bmcl.2011.11.045
  • Peer Reviewed
• [Presentation] メロジテルペノイドStrongylophorine 2および類縁体の合成研究 (2012)
  • Author(s): 及川侑也・石川裕一・及川雅人
  • Organizer: 日本化学会第92春季年会
  • Place of Presentation: 慶應義塾大学日吉キャンパス
  • Year and Date: 2012-03-26
• [Presentation] メロジテルペノイドStrongylophorine 2および類縁体の合成研究 (2012)
  • Author(s): 石川裕一
  • Organizer: 日本化学会第92春季年会
  • Place of Presentation: 横浜
  • Year and Date: 2012-03-26