Structure Activity Relationships Study of Ingenols for Novel Anti-HIV Drugs

• Project/Area Number: 24810001
• Research Category: Grant-in-Aid for Research Activity Start-up
• Allocation Type: Single-year Grants
• Research Field: Living organism molecular science
• Research Institution: University of Tsukuba
• Principal Investigator: OHYOSHI TAKAYUKI 筑波大学, 国際統合睡眠医科学研究機構, 助教 (90639303)
• Project Period (FY): 2012-08-31 – 2014-03-31
• Project Status: Completed (Fiscal Year 2013)
• Budget Amount: ¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000); Fiscal Year 2013: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000); Fiscal Year 2012: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
• Keywords: 13－オキシインゲノール / インゲノール / 構造活性相関研究 / HIV活性 / PKC活性 / 天然物化学 / 13‐オキシインゲノール / inside-outside炭素骨格 / 13-オキシインゲノール

Research Abstract

13-Oxyingenol is a diterpenoid isolated from the plants of Euphorbia sp. 13-Oxyingenol and it's derivatives have strong anti HIV activity and PKC activation. I synthesized many 13-oxyingenol derivatives and measured PKC activation. Also, I have achieved the synthesis of the tetracyclic skeleton of ingenol based on total synthesis of 13-oxyingenol.

Research Products

• [Presentation] 13-オキシインゲノール類の全合成 (2012)
  • Author(s): 大好孝幸
  • Organizer: 第2回若手研究者ワークショップ
  • Place of Presentation: 大阪大学
  • Year and Date: 2012-10-30
• [Presentation] 13-オキシインゲノール類の全合成 (2012)
  • Author(s): 大好孝幸
  • Organizer: 第54回天然有機化合物討論会
  • Place of Presentation: 東京農業大学
• [Presentation] 13-オキシインゲノール類の全合成 (2012)
  • Author(s): 大好孝幸
  • Organizer: 第56回香料・テルペンおよび精油化学に関する討論会
  • Place of Presentation: 鹿児島大学
• [Remarks]
  • URL: http://nagase.wpi-iiis.tsukuba.ac.jp/