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Development of novel drug leads based on rare tropical resources

Research Project

Project/Area Number 18H02583
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Review Section Basic Section 47050:Environmental and natural pharmaceutical resources-related
Research InstitutionKanazawa University

Principal Investigator

Goto Kyoko  金沢大学, 薬学系, 准教授 (50180245)

Co-Investigator(Kenkyū-buntansha) 三宅 克典  東京薬科大学, 薬学部, 講師 (20597687)
斎藤 洋平  金沢大学, 先進予防医学研究センター, 助教 (90723825)
Project Period (FY) 2018-04-01 – 2022-03-31
Project Status Completed (Fiscal Year 2021)
Budget Amount *help
¥17,160,000 (Direct Cost: ¥13,200,000、Indirect Cost: ¥3,960,000)
Fiscal Year 2021: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2020: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2019: ¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2018: ¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Keywords熱帯雨林産植物 / 生物活性天然物 / 熱帯資源 / 創薬リード / 生理活性天然物 / 熱帯林産植物 / 抗腫瘍活性
Outline of Final Research Achievements

Over 50 novel natural products were isolated from phytochemically untouched rainforest plants, elucidated their chemical structure, and evaluated for antiproliferative activity against tumor cell lines. The synthetic routs of bioactive natural products were developed, and various derivatives were synthesized. The structure-activity relationships and their mechanisms of action of bioactive derivatives were also investigated.

Academic Significance and Societal Importance of the Research Achievements

熱帯雨林は生物多様性に富むことが知られ、生息する植物からこれまでに多くの医薬品が誕生してきた。アメリカ国立がん研究所NCIが所有する、抗腫瘍活性を有し且つ未解析の熱帯雨林産植物エキスから単離した新規天然物、ならびに合成を通して得られた生物活性天然物誘導体は、構造多様性に富む化合物ライブラリーの拡充につながり、がんや新型感染症等に対する将来の創薬研究への寄与が期待できる。

Report

(5 results)
  • 2021 Annual Research Report   Final Research Report ( PDF )
  • 2020 Annual Research Report
  • 2019 Annual Research Report
  • 2018 Annual Research Report
  • Research Products

    (47 results)

All 2022 2021 2020 2019 2018 Other

All Int'l Joint Research (5 results) Journal Article (18 results) (of which Int'l Joint Research: 12 results,  Peer Reviewed: 18 results,  Open Access: 3 results) Presentation (24 results) (of which Int'l Joint Research: 1 results,  Invited: 2 results)

  • [Int'l Joint Research] アメリカ国立がん研究所/ノースカロライナ大学(米国)

    • Related Report
      2021 Annual Research Report
  • [Int'l Joint Research] ハサヌディン大学(インドネシア)

    • Related Report
      2021 Annual Research Report
  • [Int'l Joint Research] ノースカロライナ大学/国立がん研究所/デューク大学(米国)

    • Related Report
      2020 Annual Research Report
  • [Int'l Joint Research] ハサヌディン大学(インドネシア)

    • Related Report
      2020 Annual Research Report
  • [Int'l Joint Research] 米国国立がん研究所/ノースカロライナ大学(米国)

    • Related Report
      2018 Annual Research Report
  • [Journal Article] Chemical space expansion of flavonoids: Induction of mitotic inhibition by replacing ring-B with a 10π-electron system, benzo[b]thiophene2022

    • Author(s)
      Hirazawa S, Saito Y, Sagano M, Goto M, Nakagawa-Goto K.
    • Journal Title

      J. Nat. Prod

      Volume: 85 Issue: 1 Pages: 136-147

    • DOI

      10.1021/acs.jnatprod.1c00867

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Novel Seco-phenanthroquinolizidine Alkaloids from Indonesian Boehmeria virgata, Phytochem2021

    • Author(s)
      Rahim A, Saito Y, Miyake K, Goto M, Nakagawa-Goto K
    • Journal Title

      Phytochem. Lett.

      Volume: 45 Pages: 132-126

    • DOI

      10.1016/j.phytol.2021.08.003

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Boroxazolidone formation under physiological conditions toward chemical modification of biomolecules2021

    • Author(s)
      Saito Y, Yoshida N, Nakagawa-Goto K,
    • Journal Title

      Chem Lett

      Volume: 50 Issue: 9 Pages: 1695-1698

    • DOI

      10.1246/cl.210352

    • NAID

      130008088232

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed
  • [Journal Article] α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer2021

    • Author(s)
      Saito Y, Mizokami A, Izumi K, Naito R, Goto M, Nakagawa-Goto K
    • Journal Title

      Molecules

      Volume: 26 Issue: 9 Pages: 2812-2825

    • DOI

      10.3390/molecules26092812

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives2021

    • Author(s)
      Saito Y, Taniguchi Y, Hirazawa S, Miura Y, Tsurimoto H, Nakayoshi T, Oda A, Hamel E, Yamashita K, Goto M, Nakagawa-Goto K
    • Journal Title

      Eur. J. Med. Chem.

      Volume: 222 Pages: 113578-113578

    • DOI

      10.1016/j.ejmech.2021.113578

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Synthesis of Thio-lignane Analogue, Bioequivalent Salvinal without Unfavored Aldehyde2021

    • Author(s)
      Saito Y, Kobayashi Y, Yoshida N, Goto M, Nakagawa-Goto K
    • Journal Title

      J. Org. Chem

      Volume: 86 Issue: 10 Pages: 7092-7106

    • DOI

      10.1021/acs.joc.1c00348

    • Related Report
      2021 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Bicyclic Chalcones as Mitotic Inhibitors for Overcoming Androgen Receptor-Independent and Multidrug Resistant Prostate Cancer2021

    • Author(s)
      Saito Y, Mizokami M, Maeda S, Takahashi K, Izumi K, Goto M, Nakagawa-Goto K
    • Journal Title

      ACS Omega

      Volume: 6 Issue: 7 Pages: 4842-4849

    • DOI

      10.1021/acsomega.0c05822

    • Related Report
      2021 Annual Research Report 2020 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Novel furoquinolinones from an Indonesian Plant, Lunasia amara2020

    • Author(s)
      M. Yamashita, Y. Saito, A. Rahim, S. iFukuyoshi, K. Miyake, M. Goto, K. Nakagawa-Goto
    • Journal Title

      Tetrahedrone Lett.

      Volume: in press Issue: 20 Pages: 151861-151861

    • DOI

      10.1016/j.tetlet.2020.151861

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] First Total Synthesis of a Pavine Alkaloid, (±)-Neocaryachine, and its Optical Resolution2020

    • Author(s)
      Miura Y, Saito Y, Goto M, Nakagawa-Goto K.
    • Journal Title

      Chem. Pharm. Bull

      Volume: 68 Issue: 9 Pages: 899-902

    • DOI

      10.1248/cpb.c20-00370

    • NAID

      130007893858

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Development of an efficient scale-up synthesis for β3-adrenergic receptor agonist, ritobegron ethyl hydrochloride2020

    • Author(s)
      Sonehara J, Tamai T, Isawa H, Hotei Y, Kasai K, Kikuchi N, Ishikawa T, Kobayashi M, Ozawa T, Suzuki R, Kobayashi M, Ainai T, Nishimura M, Saito Y, Nakagawa-Goto K
    • Journal Title

      Org. Proc. Res. Dev

      Volume: 24 Issue: 9 Pages: 1675-1682

    • DOI

      10.1021/acs.oprd.0c00278

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Palasanines A-E, 3,4-Methylenedioxyquinoline Alkaloids Fused with a Phenyl-14-oxabicyclo[3.2.1]octane Unit from Melochia umbellata var. deglabrata2020

    • Author(s)
      Rahim A, Saito Y, Fukuyoshi S, Miyake K, Goto M, Chen CH, Alam G, Lee KH, Nakagawa-Goto K.
    • Journal Title

      J. Nat. Prod.

      Volume: 83 Issue: 10 Pages: 2931-2939

    • DOI

      10.1021/acs.jnatprod.0c00454

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Anti-proliferative and chemosensitizing effects of diarylheptanoids on human tumor cell lines2019

    • Author(s)
      Miyagishi S, Saito Y, Goto M, Nakagawa-Goto K
    • Journal Title

      ACS Omega

      Volume: 4 Issue: 1 Pages: 2053-2062

    • DOI

      10.1021/acsomega.8b03215

    • Related Report
      2019 Annual Research Report 2018 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Synthesis of 4-epi-parviflorons A, C, and E: structure-activity relationship study of antiproliferative abietane derivatives.2019

    • Author(s)
      Miyajima, Y.; Saito, Y.; Takeya, M.; Goto, M.; Nakagawa-Goto, K.
    • Journal Title

      The Journal of Organic Chemistry

      Volume: 84 Issue: 6 Pages: 3239-3248

    • DOI

      10.1021/acs.joc.8b02832

    • Related Report
      2019 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Spiro[3.5]nonenyl meroterpenoid lactones, cryptolaevilactones G-L, an ionone derivative and total synthesis of cryptolaevilactone M from Cryptocarya laevigata2019

    • Author(s)
      Tsurumi F, Miura Y, Nakano M, Saito Y, Fukuyoshi S, Newman DJ, O’Keefe BR, Lee KH, Nakagawa-Goto K
    • Journal Title

      J Nat Prod

      Volume: 82 Issue: 9 Pages: 2368-2378

    • DOI

      10.1021/acs.jnatprod.8b00732

    • Related Report
      2019 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Prenylated acetophloroglucinol dimers from Acronychia trifoliolata: Structure elucidation and total synthesis2019

    • Author(s)
      Miyake K, Morita C, Suzuki A, Matsushita N, Saito Y, Goto M, Newman DJ, O’Keefe BR, Lee KH, Nakagawa-Goto K
    • Journal Title

      J Nat Prod

      Volume: 82 Issue: 10 Pages: 2852-2858

    • DOI

      10.1021/acs.jnatprod.9b00596

    • Related Report
      2019 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] Isolation, Structure Elucidation, and Antiproliferative Activity of Butanolides and Lignan Glycosides from the Fruit of Hernandia nymphaeifolia2019

    • Author(s)
      Aimaiti S, Saito Y, Fukuyoshi S, Goto M, Miyake K, Newman DJ, O’Keefe BR, Lee KH, Nakagawa-Goto K
    • Journal Title

      Molecules

      Volume: 24 Issue: 21 Pages: 4005-4021

    • DOI

      10.3390/molecules24214005

    • Related Report
      2019 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research
  • [Journal Article] Antiproliferative alkaloids from Alangium longiflorum, an endangered tropical plant species2018

    • Author(s)
      Takeuchi M, Saito Y, Goto M, Miyake K, Newman DJ, O’Keefe BR, Lee KH, Nakagawa-Goto K.
    • Journal Title

      J Nat Prod

      Volume: 81 Issue: 8 Pages: 1884-1891

    • DOI

      10.1021/acs.jnatprod.8b00411

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Journal Article] 5’-Chloro-2,2’-dihydroxychalcone and Related Flavanoids as Treatments for Prostate Cancer2018

    • Author(s)
      Saito Y, Mizokami A, Tsurimoto H, Izumi K, Goto M, Nakagawa-Goto K
    • Journal Title

      Eur J Med Chem

      Volume: 157 Pages: 1143-1152

    • DOI

      10.1016/j.ejmech.2018.08.069

    • Related Report
      2018 Annual Research Report
    • Peer Reviewed / Int'l Joint Research
  • [Presentation] 抗トリプルネガティブ乳がんを志向したノルエレモフィラン誘導体の合成と構造活性相関研究2022

    • Author(s)
      中山わかな,前田 紗弥加,佐賀野 桃子,斎藤 洋平,後藤(中川)享子
    • Organizer
      日本薬学会第142年会
    • Related Report
      2021 Annual Research Report
  • [Presentation] 熱帯雨林産植物Trichilia rubescensの成分探索と生理活性評価2022

    • Author(s)
      賽旦夏阿木提,斎藤 洋平,三宅克典,David J. Newman, Barry O’Keefe,後藤(中川)享子
    • Organizer
      日本薬学会第142年会
    • Related Report
      2021 Annual Research Report
  • [Presentation] ジアリールボリン酸を利用した標的タンパク質同定法の開発2022

    • Author(s)
      田部井透矢,後藤(中川)享子,斎藤洋平
    • Organizer
      日本化学会102年会
    • Related Report
      2021 Annual Research Report
  • [Presentation] プレニルアセトフェノン二量体、アクロトリフォリオラン Aの合成研究2022

    • Author(s)
      新田夕莉,松下夏子,斎藤洋平,後藤(中川)享子
    • Organizer
      日本化学会102年会
    • Related Report
      2021 Annual Research Report
  • [Presentation] 抗腫瘍活性キノロンアルカロイドWaltherione A の全合成2021

    • Author(s)
      下井涼介,三浦悠太,斎藤洋平,後藤(中川)享子
    • Organizer
      第50回複素環化学討論会
    • Related Report
      2021 Annual Research Report
  • [Presentation] スピロ[3.5]ノナン骨格含有天然物Cryptolaevilactone類モデル化合物の合成研究2021

    • Author(s)
      三浦悠太,斎藤洋平,後藤(中川)享子
    • Organizer
      第47回反応と合成の進歩シンポジウム
    • Related Report
      2021 Annual Research Report
  • [Presentation] Drug discovery and development based on natural products2021

    • Author(s)
      後藤(中川)享子
    • Organizer
      1st Makassar International Conference in Pharmaceutical Sciences
    • Related Report
      2021 Annual Research Report
    • Int'l Joint Research / Invited
  • [Presentation] モノテルペン-ポリケチドCryptolaevilactone類の合成研究2021

    • Author(s)
      三浦悠太,斎藤洋平,後藤(中川)享子
    • Organizer
      日本薬学会第141年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] ブロモエレモフィランPC-Aの全合成と抗トリプルネガティブ乳がん選択性における構造活性相関研究2021

    • Author(s)
      前田 紗弥加,佐賀野 桃子,斎藤 洋平,後藤(中川)享子
    • Organizer
      日本薬学会第141年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] 再燃前立腺がんに有効なα置換フェニルスチリルケトン誘導体の創出と作用機序に関する研究2021

    • Author(s)
      斎藤 洋平,溝上 敦,泉 浩二,内藤 伶奈人,後藤 益生,後藤(中川)享子
    • Organizer
      日本薬学会第141年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] 生体分子の化学修飾を志向した温和な条件におけるボロキサゾリドン形成2021

    • Author(s)
      斎藤洋平,吉田菜々美,後藤(中川)享子
    • Organizer
      日本化学会第101春季年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] スピロ[3.5]ノナン骨格含有メロテルペノイドCryptolaevilactone類の全合成研究2020

    • Author(s)
      三浦悠太,斎藤洋平,後藤(中川)享子
    • Organizer
      日本薬学会第140年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] トリプルネガティブ乳がん選択的な細胞増殖抑制効果をもつエレモフィラン型セスキテルペンPC-Aの合成2020

    • Author(s)
      前田 紗弥加,佐賀野 桃子,斎藤 洋平,後藤(中川)享子
    • Organizer
      日本薬学会第140年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] 勢抵抗性前立腺がんに有効なカルコン誘導体の創出と標的タンパク質の探索2020

    • Author(s)
      斎藤 洋平,溝上 敦,泉 浩二,内藤 伶奈人,後藤 益生,後藤(中川)享子
    • Organizer
      日本薬学会第140年会
    • Related Report
      2020 Annual Research Report
  • [Presentation] 薬用生理活性天然物の単離精製・合成・メディシナルケミストリーへの展開2020

    • Author(s)
      後藤(中川)享子
    • Organizer
      日本薬学会第140年会
    • Related Report
      2020 Annual Research Report
    • Invited
  • [Presentation] Thio-salvinal 誘導体群の合成,がん細胞増殖抑制効果と構造活性相関研究2019

    • Author(s)
      吉田奈々美,小林由希子,斎藤洋平,後藤益生,後藤(中川)享子
    • Organizer
      日本薬学会第139年会
    • Related Report
      2019 Annual Research Report 2018 Annual Research Report
  • [Presentation] トリプルネガティブ乳がん選択的に増殖抑制活性を示す天然物誘導体プローブの設計と合成2019

    • Author(s)
      坂田耕一,斎藤洋平,後藤(中川)享子
    • Organizer
      日本薬学会第139年会
    • Related Report
      2019 Annual Research Report 2018 Annual Research Report
  • [Presentation] Cryptocarya laevigata由来モノテルペン-ポリケチドcryptolaevilactones A-Fの合成2019

    • Author(s)
      三浦悠太,斎藤洋平,後藤(中川)享子
    • Organizer
      日本薬学会第139年会
    • Related Report
      2019 Annual Research Report
  • [Presentation] Acronychia trifoliolata 由来の新規アセトフェノンダイマー類の合成とがん細胞増殖抑制効果2019

    • Author(s)
      松下夏子,森田千尋,斎藤洋平,後藤益生,後藤(中川)享子
    • Organizer
      日本薬学会第139年会
    • Related Report
      2019 Annual Research Report 2018 Annual Research Report
  • [Presentation] Cryptocarya laevigata由来モノテルペン-ポリケチドcryptolaevilactones A–Fの合成2019

    • Author(s)
      三浦悠太,斎藤洋平,後藤(中川)享子
    • Organizer
      日本薬学会第139年会
    • Related Report
      2018 Annual Research Report
  • [Presentation] 生理活性フラボノイドTEDB-TBのアミノ誘導体合成と活性評価2018

    • Author(s)
      斎藤 洋平,小林 佑希子,後藤 益生,後藤(中川) 享子
    • Organizer
      日本ケミカルバイオロジー学会 第 13回年会
    • Related Report
      2018 Annual Research Report
  • [Presentation] エレモフィラン型セスキテルペンPC-Aの合成とトリプルネガティブ乳がん細胞選択的増殖抑制評価2018

    • Author(s)
      佐賀野桃子,斎藤洋平,後藤益生,後藤(中川)享子
    • Organizer
      第36回メディシナルケミストリーシンポジウム
    • Related Report
      2018 Annual Research Report
  • [Presentation] ジアリールヘプタノイド誘導体のがん化学療法増感効果2018

    • Author(s)
      宮岸佐衣,斎藤洋平,後藤益生,後藤(中川)享子
    • Organizer
      第36回メディシナルケミストリーシンポジウム
    • Related Report
      2018 Annual Research Report
  • [Presentation] 各種ベンゾチオフェンフラボノイド誘導体の合成とがん細胞増殖抑制効果2018

    • Author(s)
      平澤幸香 ,谷口由花子,佐賀野桃子,斎藤洋平,後藤益生,後藤(中川)享子
    • Organizer
      第36回メディシナルケミストリーシンポジウム
    • Related Report
      2018 Annual Research Report

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Published: 2018-04-23   Modified: 2023-01-30  

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