Sugar chain targeting symmetrical boronic acid derivatives

• Project/Area Number: 17K15486
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Drug development chemistry
• Research Institution: Fukuoka University
• Principal Investigator: Furutachi Makoto 福岡大学, 薬学部, 助教 (30759931)
• Project Period (FY): 2017-04-01 – 2019-03-31
• Project Status: Completed (Fiscal Year 2018)
• Budget Amount: ¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000); Fiscal Year 2018: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000); Fiscal Year 2017: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
• Keywords: 創薬 / 生物活性 / 糖鎖 / C2対称 / ボロン酸

Outline of Final Research Achievements

Biological activity of synthesized compounds was evaluated and some compounds showed antibacterial, antiviral, and cytotoxic activities. The anticancer activity of compounds that showed cytotoxic activity was evaluated using human brain cancer cells and human head and neck cancer cells. All of the synthesized compounds showed lower anticancer activity toward human brain cancer cells than that of the positive control drug cisplatin, but one synthesized compound showed higher anticancer activity toward human head and neck cancer cells than that of cisplatin.

Academic Significance and Societal Importance of the Research Achievements

本研究では、多剤耐性菌や多剤耐性ウイルスの出現により需要の高まる、新たな抗菌薬および抗ウイルス薬の創製へと繋がる可能性のある化合物を創出した。また、社会的要請の大きい、新たな抗悪性腫瘍薬の創製へと繋がる可能性のある化合物を探索し、既存の抗悪性腫瘍薬シスプラチンよりも抗腫瘍活性の強い化合物を創出した。

Research Products

• [Journal Article] Anti-proliferative Activities Towards Human Brain Glioma U251 Cells and Human Carcinoma Cells (KB3-1) of Some Twin-Drug Type Bivalent C2-Symmetrical Phenylboronic Acid Derivatives (2019)
  • Author(s): Furutachi M., Gondo T., Ikeda R., Yoshikawa N., Yokota T., Takeda Y., Yokomizo K., Zhou J.-R., Kashige N., Miake F., Sumoto K.
  • Journal Title: Biol. Pharm. Bull. Volume: in press
  • NAID: 130007641479
• [Journal Article] Novel Trivalent C3-Symmetrical Phenylboronic Acid Pinacol Esters and Their Biological Evaluation (2018)
  • Author(s): Furutachi M., Fuchigami S., Ako K., Goto S., Gondo T., Takuse M., Yoshida M., Yokomizo K., Zhou J.-R., Matsunaga A., Hiraga N., Kashige N., Miake F., Sumoto K.
  • Journal Title: Heterocycles Volume: 96 Issue: 1 Pages: 144-151
  • DOI: 10.3987/com-17-13832
  • Peer Reviewed
• [Journal Article] Preparation of Novel Bivalent Linker Mode Phenylboronic Acid Derivatives and Their Biological Evaluation (2018)
  • Author(s): Furutachi M., Matsumoto A., Tamenaga T., Sugita A., Kuroiwa M., Yokomizo K., Zhou J.-R., Kashige N., Miake F., Sumoto K.
  • Journal Title: Heterocycles Volume: 96 Issue: 6 Pages: 1088-1100
  • DOI: 10.3987/com-18-13899
  • NAID: 40021581294
  • Peer Reviewed
• [Journal Article] Novel C2-Symmetrical Phenylboronic Acid Pinacol Esters with a Few Types of Linkers and Their Biological Activities (2017)
  • Author(s): Furutachi M., Gondo T., Goto S., Fuchigami S., Ako K., Oowada Y., Yokomizo K., Zhou J.-R., Ishizaki T., Koga T., Kashige N., Miake F., Sumoto K.
  • Journal Title: Heterocycles Volume: 94 Issue: 9 Pages: 1748-1758
  • DOI: 10.3987/com-17-13745
  • Peer Reviewed
• [Presentation] トリバレントC3対称性フェニルボロン酸の合成と生物活性 (2019)
  • Author(s): 古舘信、牛島由紀子、池廣裕馬、稲田智美、周建融、横溝和美、鹿志毛信広、見明史雄、須本國弘
  • Organizer: 日本薬学会第139年会(千葉)
• [Presentation] N-アシルアミノ置換フェニルボロン酸誘導体の合成とその生物活性：1価及び多価フェニルボロン酸誘導体類の生物活性の比較 (2018)
  • Author(s): 爲永徹也、古舘信、周建融、松永綾、平賀希、横溝和美、鹿志毛信広、見明史雄、須本國弘
  • Organizer: 日本薬学会第138年会(金沢)
• [Presentation] Preparation and Biological Activity of Symmetrical Phenylboronic Acid Derivatives (2018)
  • Author(s): Furutachi M., Yokomizo K., Zhou J.-R., Kashige N., Miake F., Sumoto K.
  • Organizer: 17th Annual World Preclinical Congress (Boston, United States)
  • Int'l Joint Research
• [Presentation] N-アシルアミノ置換フェニルボロン酸誘導体の合成とその生物活性：1価及び多価フェニルボロン酸誘導体類の生物活性の比較 (2018)
  • Author(s): 爲永徹也、古舘信、周建融、松永綾、平賀希、横溝和美、鹿志毛信広、見明史雄、須本國弘
  • Organizer: 日本薬学会第138年会
• [Remarks]
  • URL: http://tyufghjvbn.wixsite.com/tyufghjvbn