• Search Research Projects
  • Search Researchers
  • How to Use
  1. Back to previous page

Structure-anticancer activity relationship study of natural product and its derivatives with a novel mechanism of action

Research Project

Project/Area Number 25860015
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Chemical pharmacy
Research InstitutionMeiji Pharmaceutical University

Principal Investigator

Kobayashi Kenichi  明治薬科大学, 薬学部, 助教 (30639282)

Project Period (FY) 2013-04-01 – 2016-03-31
Project Status Completed (Fiscal Year 2015)
Budget Amount *help
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2013: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
KeywordsPhaeosphaeride A / 天然物の全合成 / 抗がん剤 / 構造活性相関
Outline of Final Research Achievements

Phaeosphaeride A, a natural product isolated from an endophytic fungus in 2006, inhibits the STAT3-dependent signaling. Thus, this natural product is expected to be a seed compound for developing an anticancer chemotherapeutic agent.
In this study, first total synthesis of phaeosphaeride A was achieved, and its stereostructures including the relative and absolute configurations were established. Its enantiomer, diastereomer, and some artifacts were also prepared for the sturucture-activity relationship study.

Report

(4 results)
  • 2015 Annual Research Report   Final Research Report ( PDF )
  • 2014 Research-status Report
  • 2013 Research-status Report
  • Research Products

    (23 results)

All 2016 2015 2014 2013 Other

All Journal Article (2 results) (of which Peer Reviewed: 2 results) Presentation (20 results) (of which Int'l Joint Research: 1 results) Remarks (1 results)

  • [Journal Article] Establishment of Relative and Absolute Configurations of Phaeosphaeride A: Total Synthesis of ent-Phaeosphaeride A2015

    • Author(s)
      Kenichi Kobayashi, Yukiko Kobayashi, Misato Nakamura, Osamu Tamura, and Hiroshi Kogen
    • Journal Title

      The Journal of Organic Chemistry

      Volume: 80 Issue: 2 Pages: 1243-1248

    • DOI

      10.1021/jo5025046

    • Related Report
      2014 Research-status Report
    • Peer Reviewed
  • [Journal Article] Studies toward the Second-Generation Synthesis of Epolactaene: Highly Stereoselective Construction of the Epoxy-γ-Lactam Moiety2014

    • Author(s)
      Kouta Tajima, Yoshifumi Umehara, Kenichi Kobayashi, Hiroshi Kogen
    • Journal Title

      Synlett

      Volume: 25 Issue: 16 Pages: 2337-2340

    • DOI

      10.1055/s-0034-1378562

    • Related Report
      2014 Research-status Report
    • Peer Reviewed
  • [Presentation] Darzens縮合を用いたepoxy-γ-lactam環の効率的合成法の開発2016

    • Author(s)
      田中耕作三世、小林健一、古源寛
    • Organizer
      日本薬学会第136年会(横浜)
    • Place of Presentation
      パシフィコ横浜(神奈川県横浜市)
    • Year and Date
      2016-03-26
    • Related Report
      2015 Annual Research Report
  • [Presentation] 光学活性な2α,2α-二置換インドールの新規合成法の開発2016

    • Author(s)
      五江渕祐太、春田雄太郎、小林健一、古源寛
    • Organizer
      日本薬学会第136年会(横浜)
    • Place of Presentation
      パシフィコ横浜(神奈川県横浜市)
    • Year and Date
      2016-03-26
    • Related Report
      2015 Annual Research Report
  • [Presentation] DGAT-1阻害剤のデザイン、合成、及び活性評価2016

    • Author(s)
      松下航平、平野遼太郎、森若菜、郡司幸恵、小林健一、古源寛、若杉昌輝、広野修一、白波瀬弘明
    • Organizer
      日本薬学会第136年会(横浜)
    • Place of Presentation
      パシフィコ横浜(神奈川県横浜市)
    • Year and Date
      2016-03-26
    • Related Report
      2015 Annual Research Report
  • [Presentation] 抗菌活性物質biverlactone Cの全合成研究2016

    • Author(s)
      桑原佳佑、小林健一、古源寛
    • Organizer
      日本薬学会第136年会(横浜)
    • Place of Presentation
      パシフィコ横浜(神奈川県横浜市)
    • Year and Date
      2016-03-26
    • Related Report
      2015 Annual Research Report
  • [Presentation] Relative and Absolute Configurations of Phaeosphaeride A: Total Synthesis of ent-Phaeosphaeride A2015

    • Author(s)
      Kenichi Kobayashi, Yukiko Kobayashi, Misato Nakamura, Osamu Tamura, Hiroshi Kogen
    • Organizer
      PACIFICHEM 2015
    • Place of Presentation
      Honolulu, Hawaii, USA
    • Year and Date
      2015-12-15
    • Related Report
      2015 Annual Research Report
    • Int'l Joint Research
  • [Presentation] Phaeosphaeride Aの相対および絶対立体配置の決定2015

    • Author(s)
      小林健一、小林夕貴子、中村美里、田村修、古源寛
    • Organizer
      日本薬学会第135年会(神戸)
    • Place of Presentation
      デザイン・クリエイティブセンター神戸
    • Year and Date
      2015-03-27
    • Related Report
      2014 Research-status Report
  • [Presentation] sp2 C-Br/C-H型クロスカップリング反応を利用したBractelactoneの全合成研究2015

    • Author(s)
      小林健一、中村美里、高橋恵美、古源寛
    • Organizer
      日本薬学会第135年会(神戸)
    • Place of Presentation
      デザイン・クリエイティブセンター神戸
    • Year and Date
      2015-03-27
    • Related Report
      2014 Research-status Report
  • [Presentation] DGAT-1阻害に基づく糖尿病治療薬の合成研究2015

    • Author(s)
      森若菜、平野遼太郎、郡司幸恵、小林健一、古源寛、若杉昌輝、広野修一、白波瀬弘明
    • Organizer
      日本薬学会第135年会(神戸)
    • Place of Presentation
      デザイン・クリエイティブセンター神戸
    • Year and Date
      2015-03-27
    • Related Report
      2014 Research-status Report
  • [Presentation] ent-Phaeosphaeride Aの全合成2014

    • Author(s)
      小林健一、小林夕貴子、田村修、古源寛
    • Organizer
      第58回日本薬学会関東支部大会
    • Place of Presentation
      昭和薬科大学
    • Year and Date
      2014-10-04
    • Related Report
      2014 Research-status Report
  • [Presentation] First Total Synthesis of ent-Phaeosphaeride A2014

    • Author(s)
      Kenichi Kobayashi, Yukiko Kobayashi, Osamu Tamura, Hiroshi Kogen
    • Organizer
      24th French-Japanese Symposium on Medicinal and Fine Chemistry
    • Place of Presentation
      Lyon, France
    • Year and Date
      2014-09-15
    • Related Report
      2014 Research-status Report
  • [Presentation] Synthetic Studies on L-755,807, a Non-Peptide Bradykinin Antagonist2014

    • Author(s)
      Kosaku III Tanaka, Kenichi Kobayashi, Hiroshi Kogen
    • Organizer
      24th French-Japanese Symposium on Medicinal and Fine Chemistry
    • Place of Presentation
      Lyon, France
    • Year and Date
      2014-09-15
    • Related Report
      2014 Research-status Report
  • [Presentation] Phaeosphaeride Aの全合成研究2014

    • Author(s)
      小林健一、田村修、古源寛
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] エポチロンDの全合成研究2014

    • Author(s)
      鈴木詩織、橋本昭吾、小林健一、古源寛
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] 2α,2α-二置換インドールの新規合成法の開発2014

    • Author(s)
      春田雄太郎、北野翔大、小林健一、古源寛
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] 神経突起伸長誘導物質エポラクタエンの第二世代合成法の開発研究2014

    • Author(s)
      田島広大、梅原義史、中田亜紀子、小林健一、古源寛
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本市総合体育館
    • Related Report
      2013 Research-status Report
  • [Presentation] 糖尿病治療薬を指向したDGAT-1阻害剤のデザイン、合成及び活性評価2014

    • Author(s)
      平野遼太郎、小林健一、古源寛、若杉昌輝、広野修一、國代一祥
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本大学工学部2号館
    • Related Report
      2013 Research-status Report
  • [Presentation] L-755,807の全合成研究2014

    • Author(s)
      田中耕作三世、小林健一、古源寛
    • Organizer
      日本薬学会第134年会
    • Place of Presentation
      熊本大学全学教育棟
    • Related Report
      2013 Research-status Report
  • [Presentation] ジアシルグリセロールアシル基転位酵素-1阻害剤のLigand-Based Drug Design2013

    • Author(s)
      若杉昌輝、合田浩明、平野遼太郎、小林健一、古源寛、広野修一
    • Organizer
      第41回構造活性相関シンポジウム
    • Place of Presentation
      関西学院会館
    • Related Report
      2013 Research-status Report
  • [Presentation] Studies toward the total synthesis of L-755,8072013

    • Author(s)
      K. Tanaka, K. Kobayashi, H. Kogen
    • Organizer
      The 23rd FRENCH-JAPANESE SYMPOSIUM on Medical and Fine Chemistry
    • Place of Presentation
      ANA CROWNE PLAZA NAGASAKI GLOVERHILL
    • Related Report
      2013 Research-status Report
  • [Presentation] Total synthesis and biological evaluations of an aplyronine A-mycalolide B hybrid2013

    • Author(s)
      K. Kobayashi, H. Kogen, I. Hayakawa, H. Kigoshi
    • Organizer
      1st European Conference on Natural Products
    • Place of Presentation
      DECHEMA-HAUS, Frankfurt, Germany
    • Related Report
      2013 Research-status Report
  • [Remarks] 明治薬科大学 医薬分子設計学教室ホームページ

    • URL

      http://www.my-pharm.ac.jp/~ph-mo-ds/index.html

    • Related Report
      2015 Annual Research Report 2014 Research-status Report

URL: 

Published: 2014-07-25   Modified: 2019-07-29  

Information User Guide FAQ News Terms of Use Attribution of KAKENHI

Powered by NII kakenhi