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Sugar chain targeting symmetrical boronic acid derivatives

Research Project

Project/Area Number 17K15486
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionFukuoka 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 *help
¥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。

Report

(3 results)
  • 2018 Annual Research Report   Final Research Report ( PDF )
  • 2017 Research-status Report
  • Research Products

    (9 results)

All 2019 2018 2017 Other

All Journal Article (4 results) (of which Peer Reviewed: 3 results) Presentation (4 results) (of which Int'l Joint Research: 1 results) Remarks (1 results)

  • [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 Derivatives2019

    • 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

    • Related Report
      2018 Annual Research Report
  • [Journal Article] Novel Trivalent C3-Symmetrical Phenylboronic Acid Pinacol Esters and Their Biological Evaluation2018

    • 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

    • Related Report
      2018 Annual Research Report 2017 Research-status Report
    • Peer Reviewed
  • [Journal Article] Preparation of Novel Bivalent Linker Mode Phenylboronic Acid Derivatives and Their Biological Evaluation2018

    • 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

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Novel C2-Symmetrical Phenylboronic Acid Pinacol Esters with a Few Types of Linkers and Their Biological Activities2017

    • 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

    • Related Report
      2017 Research-status Report
    • 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)
    • Related Report
      2018 Annual Research Report
  • [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)
    • Related Report
      2018 Annual Research Report
  • [Presentation] Preparation and Biological Activity of Symmetrical Phenylboronic Acid Derivatives2018

    • Author(s)
      Furutachi M., Yokomizo K., Zhou J.-R., Kashige N., Miake F., Sumoto K.
    • Organizer
      17th Annual World Preclinical Congress (Boston, United States)
    • Related Report
      2018 Annual Research Report
    • 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
    • Related Report
      2017 Research-status Report
  • [Remarks]

    • URL

      http://tyufghjvbn.wixsite.com/tyufghjvbn

    • Related Report
      2017 Research-status Report

URL: 

Published: 2017-04-28   Modified: 2020-03-30  

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