Fundamentals of multi-elemental medicinal chemistry for developing the novel and innovative drug candidates

• Project/Area Number: 17H03997
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Tokyo Medical and Dental University (2019-2021); The University of Tokyo (2017-2018)
• Principal Investigator: Fujii Shinya 東京医科歯科大学, 生体材料工学研究所, 准教授 (60389179)
• Project Period (FY): 2017-04-01 – 2022-03-31
• Project Status: Completed (Fiscal Year 2021)
• Budget Amount: ¥17,810,000 (Direct Cost: ¥13,700,000、Indirect Cost: ¥4,110,000); Fiscal Year 2021: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000); Fiscal Year 2020: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000); Fiscal Year 2019: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000); Fiscal Year 2018: ¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000); Fiscal Year 2017: ¥2,860,000 (Direct Cost: ¥2,200,000、Indirect Cost: ¥660,000)
• Keywords: 創薬化学 / 多元素創薬化学 / 構造物性相関 / 構造活性相関 / ホウ素 / ケイ素 / リン / 有機金属化合物 / 元素化学 / 多元素有機化合物 / メタロセン / 医薬分子設計 / 医薬品化学

Outline of Final Research Achievements

From the perspective of periodic table of elements in medicinal chemistry, structure-property relationships and structure-activity relationships of a series of multi-elemental organic compounds were systematically investigated. Structural development using a wide variety of multi-elemental compounds including silyl functionalities, phosphorus functionalities, and ferrocene were investigated to clarify the utility of these chemical species. Novel and unique ligands for androgen receptor, estrogen receptor, and progesterone receptor were developed, and novel applications of the multi-elemental species in medicinal chemistry were proposed.

Academic Significance and Societal Importance of the Research Achievements

革新的な医薬化合物の開発には、新規創薬標的の探索や新しい合成手法の開発と並んで、化合物の構造および物性的な革新性を創出する新規ケミカルスペースの開拓も有効と考える。本研究では、種々のヘテロ原子を有する多元素有機化合物が創出するケミカルスペースに着目、低分子創薬における有用性を明らかにし、その応用法を提案した。抗体医薬や核酸医薬が脚光を集める今日においても、新規低分子医薬品の開発はグローバルな医療において最も重要な領域の一つである。周期表横断的なアプローチで新たな低分子医薬化合物の設計手法を提案する本研究は、今後の革新的医薬品の創製に貢献するものと考える。

Research Products

• [Journal Article] Structural Development of Silicon‐Containing Retinoids: Structure?Activity Relationship Study of the Hydrophobic Pharmacophore of Retinobenzoic Acids Using Silyl Functionalities (2022)
  • Author(s): Oikawa Tsuyoshi、Fujii Shinya、Mori Shuichi、Masuno Hiroyuki、Kawachi Emiko、Kagechika Hiroyuki
  • Journal Title: ChemMedChem Volume: in press Issue: 12
  • DOI: 10.1002/cmdc.202200176
  • Peer Reviewed
• [Journal Article] Design, synthesis and structure?activity relationship of 4-(1,1,1,3,3,3-hexafluoro-2-hydroxyisoprop-2-yl)phenylsilane derivatives as liver X receptor agonists (2022)
  • Author(s): Namba Nao、Noguchi-Yachide Tomomi、Matsumoto Yuichiro、Hashimoto Yuichi、Fujii Shinya
  • Journal Title: Bioorganic and Medicinal Chemistry Volume: 66 Pages: 116792-116792
  • DOI: 10.1016/j.bmc.2022.116792
  • Peer Reviewed
• [Journal Article] Design, synthesis and antitumor activity of phthalazine-1,4-dione-based menaquinone analogs (2021)
  • Author(s): Fujii Shinya、Miura Takahiro、Oikawa Tsuyoshi、Qin Xian-Yang、Kojima Soichi、Kagechika Hiroyuki
  • Journal Title: Bioorganic and Medicinal Chemistry Letters Volume: 43 Pages: 128065-128065
  • DOI: 10.1016/j.bmcl.2021.128065
  • Peer Reviewed
• [Journal Article] Structure-property and structure?activity relationships of phenylferrocene derivatives as androgen receptor antagonists (2021)
  • Author(s): Ochiai Kotaro、Fujii Shinya
  • Journal Title: Bioorganic and Medicinal Chemistry Letters Volume: 46 Pages: 128141-128141
  • DOI: 10.1016/j.bmcl.2021.128141
  • Peer Reviewed
• [Journal Article] Structural Development of Salicylanilide‐Based SPAK Inhibitors as Candidate Antihypertensive Agents (2021)
  • Author(s): Fujii Shinya、Kikuchi Eriko、Suzuyama Honoka、Watanabe Yuko、Ishigami‐Yuasa Mari、Masuno Hiroyuki、Mori Takayasu、Isobe Kiyoshi、Uchida Shinichi、Kagechika Hiroyuki
  • Journal Title: ChemMedChem Volume: 16 Issue: 18 Pages: 2817-2822
  • DOI: 10.1002/cmdc.202100273
  • Peer Reviewed
• [Journal Article] Construction of Aromatic Multilayered Structures Based on the Conformational Properties of N,N’-Dimethylated Squaramide (2021)
  • Author(s): Arimura, M.; Tanaka, K.; Kanda, M.; Urushibara, K.; Fujii, S.; Katagiri, K.; Azumaya, I.; Kagechika, H.; Tanatani, A.
  • Journal Title: ChemPlusChem Volume: 86 Issue: 1 Pages: 198-205
  • DOI: 10.1002/cplu.202000678
  • Peer Reviewed
• [Journal Article] Synthesis and structure-activity relationship study of 1,12-dicarba-closo-dodecaborane-based triol derivatives as novel nonsecosteroidal vitamin D analogs. (2021)
  • Author(s): Fujii, S.; Kano, A.; Sekine R.; Emiko K.; Kagechika, H.
  • Journal Title: Heterocycles Volume: 103 Issue: 1 Pages: 444-444
  • DOI: 10.3987/com-20-s(k)30
  • Peer Reviewed
• [Journal Article] Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer (2020)
  • Author(s): Endo Satoshi、Oguri Hiroaki、Segawa Jin、Kawai Mina、Hu Dawei、Xia Shuang、Okada Takuya、Irie Katsumasa、Fujii Shinya、Gouda Hiroaki、Iguchi Kazuhiro、Matsukawa Takuo、Fujimoto Naohiro、Nakayama Toshiyuki、Toyooka Naoki、Matsunaga Toshiyuki、Ikari Akira
  • Journal Title: Journal of Medicinal Chemistry Volume: 63 Issue: 18 Pages: 10396-10411
  • DOI: 10.1021/acs.jmedchem.0c00939
  • Peer Reviewed
• [Journal Article] Development of Androgen-Antagonistic Coumarinamides with a Unique Aromatic Folded Pharmacophore (2020)
  • Author(s): Koga, H.; Negishi, M.; Kinoshita, M.; Fujii, S.; Mori, S.; Ishigami-Yuasa, M.; Kawachi, E.; Kagechika, H.; Tanatani, A.
  • Journal Title: Int. J. Mol. Sci. Volume: 21 Issue: 15 Pages: 5584-5584
  • DOI: 10.3390/ijms21155584
  • Peer Reviewed / Open Access
• [Journal Article] Structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK inhibitors blocking WNK kinase signaling (2020)
  • Author(s): Fujii Shinya、Kikuchi Eriko、Watanabe Yuko、Suzuyama Honoka、Ishigami-Yuasa Mari、Mori Takayasu、Isobe Kiyoshi、Uchida Shinichi、Kagechika Hiroyuki
  • Journal Title: Bioorganic & Medicinal Chemistry Letters Volume: 30 Issue: 17 Pages: 127408-127408
  • DOI: 10.1016/j.bmcl.2020.127408
  • Peer Reviewed
• [Journal Article] リン官能基を用いた創薬化学研究の現状と新たな展開 (2020)
  • Author(s): 藤井 晋也
  • Journal Title: ファルマシア Volume: 56 Pages: 406-410
  • NAID: 130007841813
• [Journal Article] Phosphine boranes as less hydrophobic building blocks than alkanes and silanes: Structure-property relationship and estrogen-receptor-modulating potency of 4-phosphinophenol derivatives (2020)
  • Author(s): Saito Hiroki、Matsumoto Yuichiro、Hashimoto Yuichi、Fujii Shinya
  • Journal Title: Bioorganic & Medicinal Chemistry Volume: 28 Issue: 4 Pages: 115310-115310
  • DOI: 10.1016/j.bmc.2020.115310
  • Peer Reviewed
• [Journal Article] Development of Boron-Cluster-Based Progesterone Receptor Antagonists Bearing a Pentafluorosulfanyl (SF₅) Group (2019)
  • Author(s): Mori Shuichi、Tsuemoto Nozomi、Kasagawa Tomoya、Nakano Eiichi、Fujii Shinya、Kagechika Hiroyuki
  • Journal Title: Chemical and Pharmaceutical Bulletin Volume: 67 Issue: 12 Pages: 1278-1283
  • DOI: 10.1248/cpb.c19-00522
  • NAID: 130007754093
  • ISSN: 0009-2363, 1347-5223
  • Year and Date: 2019-12-01
  • Peer Reviewed
• [Journal Article] Design, Synthesis and Biological Evaluation of Novel Nonsteroidal Progesterone Receptor Antagonists Based on Phenylamino-1,3,5-triazine Scaffold (2019)
  • Author(s): Kaitoh Kazuma、Nakatsu Aki、Mori Shuichi、Kagechika Hiroyuki、Hashimoto Yuichi、Fujii Shinya
  • Journal Title: Chemical and Pharmaceutical Bulletin Volume: 67 Issue: 6 Pages: 566-575
  • DOI: 10.1248/cpb.c19-00094
  • NAID: 130007657391
  • ISSN: 0009-2363, 1347-5223
  • Year and Date: 2019-06-01
  • Peer Reviewed
• [Journal Article] Development of novel lithocholic acid derivatives as vitamin D receptor agonists (2019)
  • Author(s): Masuno Hiroyuki、Kazui Yuko、Tanatani Aya、Fujii Shinya、Kawachi Emiko、Ikura Teikichi、Ito Nobutoshi、Yamamoto Keiko、Kagechika Hiroyuki
  • Journal Title: Bioorganic & Medicinal Chemistry Volume: 27 Issue: 16 Pages: 3674-3681
  • DOI: 10.1016/j.bmc.2019.07.003
  • Peer Reviewed
• [Journal Article] Spontaneous chiral resolution of N,N′-diarylsquaramides: Formation of various types of one-handed helical networks during crystallization (2019)
  • Author(s): Kanda Midori、Urushibara Ko、Park Soyoung、Fujii Shinya、Masu Hyuma、Katagiri Kosuke、Azumaya Isao、Kagechika Hiroyuki、Tanatani Aya
  • Journal Title: Tetrahedron Volume: 75 Issue: 19 Pages: 2771-2777
  • DOI: 10.1016/j.tet.2019.03.049
  • Peer Reviewed
• [Journal Article] A new LC-MS assay for the quantitative analysis of vitamin K metabolites in human urine (2019)
  • Author(s): McDonald Matthew G.、Yeung Catherine K.、Teitelbaum Aaron M.、Johnson Amanda L.、Fujii Shinya、Kagechika Hiroyuki、Rettie Allan E.
  • Journal Title: Journal of Lipid Research Volume: 60 Issue: 4 Pages: 892-899
  • DOI: 10.1194/jlr.d087916
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Design and Synthesis of Cyclohexenyl-p-carborane Derivatives as a New Class of Progesterone Receptor Antagonists (2019)
  • Author(s): Kagechika Hiroyuki、Fujii Shinya、Yanagida Naoki、Mori Shuichi、Kawachi Emiko
  • Journal Title: HETEROCYCLES Volume: 99 Issue: 1 Pages: 425-425
  • DOI: 10.3987/com-18-s(f)38
  • Peer Reviewed
• [Journal Article] Structure-activity relationship of novel (benzoylaminophenoxy)phenol derivatives as anti-prostate cancer agents (2018)
  • Author(s): Kazui Yuko、Fujii Shinya、Yamada Ayumi、Ishigami-Yuasa Mari、Kagechika Hiroyuki、Tanatani Aya
  • Journal Title: Bioorganic & Medicinal Chemistry Volume: 26 Issue: 18 Pages: 5118-5127
  • DOI: 10.1016/j.bmc.2018.09.008
  • Peer Reviewed / Open Access
• [Journal Article] Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity. (2018)
  • Author(s): Toyama H, Shirakawa H, Komai M, Hashimoto Y, Fujii S.
  • Journal Title: Bioorg. Med. Chem. Volume: 26 Issue: 15 Pages: 4493-4501
  • DOI: 10.1016/j.bmc.2018.07.038
  • Peer Reviewed
• [Journal Article] Development of biotin-retinoid conjugates as chemical probes for analysis of retinoid function (2018)
  • Author(s): Fujii Shinya、Mori Shuichi、Kagechika Hiroyuki、Mendoza Parra Marco Antonio、Gronemeyer Hinrich
  • Journal Title: Bioorganic & Medicinal Chemistry Letters Volume: 28 Issue: 14 Pages: 2442-2445
  • DOI: 10.1016/j.bmcl.2018.06.011
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Efficient Lead Finding, Activity Enhancement and Preliminary Selectivity Control of Nuclear Receptor Ligands Bearing a Phenanthridinone Skeleton (2018)
  • Author(s): Nishiyama Yuko、Fujii Shinya、Makishima Makoto、Hashimoto Yuichi、Ishikawa Minoru
  • Journal Title: International Journal of Molecular Sciences Volume: 19 Issue: 7 Pages: 2090-2090
  • DOI: 10.3390/ijms19072090
  • Peer Reviewed / Open Access
• [Journal Article] Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton (2018)
  • Author(s): Nishiyama Yuko、Mori Shuichi、Makishima Makoto、Fujii Shinya、Kagechika Hiroyuki、Hashimoto Yuichi、Ishikawa Minoru
  • Journal Title: ACS Medicinal Chemistry Letters Volume: 9 Issue: 7 Pages: 641-645
  • DOI: 10.1021/acsmedchemlett.8b00058
  • Peer Reviewed
• [Journal Article] Novel androgen receptor full antagonists: Design, synthesis, and a docking study of glycerol and aminoglycerol derivatives that contain p -carborane cages (2018)
  • Author(s): Kaise Asako、Ohta Kiminori、Fujii Shinya、Oda Akifumi、Goto Tokuhito、Endo Yasuyuki
  • Journal Title: Bioorganic & Medicinal Chemistry Volume: 26 Issue: 13 Pages: 3805-3811
  • DOI: 10.1016/j.bmc.2018.06.007
  • Peer Reviewed
• [Journal Article] Structural Development of Tetrachlorophthalimides as Liver X Receptor β (LXRβ)-Selective Agonists with Improved Aqueous Solubility (2018)
  • Author(s): Sayaka Nomura, Kaori Endo-Umeda, Shinya Fujii, Makoto Makishima, Yuichi Hashimoto, Minoru Ishikawa
  • Journal Title: Bioorganic & Medicinal Chemistry Letters Volume: 28 Issue: 4 Pages: 796-801
  • DOI: 10.1016/j.bmcl.2017.12.024
  • Peer Reviewed
• [Journal Article] Development of nonsteroidal glucocorticoid receptor modulators based on N -benzyl- N -(4-phenoxyphenyl)benzenesulfonamide scaffold (2017)
  • Author(s): Yoshioka Hiromasa、Yamada Ayumi、Nishiyama Yuko、Kagechika Hiroyuki、Hashimoto Yuichi、Fujii Shinya
  • Journal Title: Bioorganig and Medicinal Chemistry Volume: 25 Issue: 13 Pages: 3461-3470
  • DOI: 10.1016/j.bmc.2017.04.032
  • Peer Reviewed
• [Journal Article] Development of WNK signaling inhibitors as a new class of antihypertensive drugs (2017)
  • Author(s): Ishigami-Yuasa Mari、Watanabe Yuko、Mori Takayasu、Masuno Hiroyuki、Fujii Shinya、Kikuchi Eriko、Uchida Shinichi、Kagechika Hiroyuki
  • Journal Title: Bioorganic & Medicinal Chemistry Volume: 25 Issue: 14 Pages: 3845-3852
  • DOI: 10.1016/j.bmc.2017.05.034
  • Peer Reviewed
• [Journal Article] Novel Non-steroidal Progesterone Receptor Ligands Based on <i>m</i>-Carborane Containing a Secondary Alcohol: Effect of Chirality on Ligand Activity (2017)
  • Author(s): Mori, S.; Takagaki, R.; Fujii, S.; Urushibara, K.; Tanatani, A.; Kagechika, H.
  • Journal Title: Chemical and Pharmaceutical Bulletin Volume: 65 Issue: 11 Pages: 1051-1057
  • DOI: 10.1248/cpb.c17-00544
  • NAID: 130006191500
  • ISSN: 0009-2363, 1347-5223
  • Peer Reviewed
• [Journal Article] Progress in the medicinal chemistry of silicon. -C/Si-Exchange and beyond- (2017)
  • Author(s): Fujii, S.,* Hashimoto, Y.
  • Journal Title: Future Med. Chem. Volume: in press Issue: 5 Pages: 485-505
  • DOI: 10.4155/fmc-2016-0193
  • Peer Reviewed
• [Presentation] 含ケイ素化合物の構造展開によるLXRβ選択的リガンドの創製 (2022)
  • Author(s): 難波奈央，谷内出友美，松本雄一朗，橋本祐一，影近弘之，藤井晋也．
  • Organizer: 日本薬学会第142年会
• [Presentation] 二置換フェロセン誘導体の構造展開による新規アンドロゲン受容体アンタゴニストの創製 (2022)
  • Author(s): 落合幸太郎，影近弘之，藤井晋也．
  • Organizer: 日本薬学会第142年会
• [Presentation] Development of silanol-based bisphenols as subtype-selective estrogen receptor modulators. (2021)
  • Author(s): Fujii, S., Matsumoto, Y., Hashimoto, Y.
  • Organizer: 19th International Symposium on Silicon Chemistry
  • Int'l Joint Research
• [Presentation] Development of Androgen Receptor Ligands Bearing Ferrocene as the Hydrophobic Pharmacophore. (2021)
  • Author(s): Ochiai, K., Kagechika, H., Fujii S.
  • Organizer: AFMC International Medicinal Chemistry Symposium 2021
  • Int'l Joint Research
• [Presentation] Development of Subtype-Selective Liver X Receptor (LXR) Ligands Using Silicon Functionalities. (2021)
  • Author(s): Namba, N., Matsumoto, Y., Hashimoto, Y., Noguchi-Yachide, T., Kagechika, H., Fujii S.
  • Organizer: AFMC International Medicinal Chemistry Symposium 2021
  • Int'l Joint Research
• [Presentation] Systematic investigation of the structure-property and structure-activity relationships of 4-phosphinophenol derivatives: Throwing light on the potential utility of phosphorus in drug discovery. (2021)
  • Author(s): Fujii, S., Saito, H., Matsumoto, Y., Hashimoto, Y., Kagechika, H.
  • Organizer: The 6th International Symposium on Biomedical Engineering
  • Int'l Joint Research
• [Presentation] Design, Synthesis and Evaluation of Novel Androgen Receptor Ligand Bearing Ferrocene as the Hydrophobic Pharmacophore (2021)
  • Author(s): Ochiai, K., Kagechika, H., Fujii, S.
  • Organizer: The 6th International Symposium on Biomedical Engineering
  • Int'l Joint Research
• [Presentation] Structure Development of Silicon-Containing Derivatives of T0901317 as Novel Liver X Receptor (LXR) Ligands. (2021)
  • Author(s): Namba, N., Matsumoto, Y., Hashimoto, Y., Noguchi-Yachide, T., Kagechika, H., Fujii, S.
  • Organizer: The 6th International Symposium on Biomedical Engineering
  • Int'l Joint Research
• [Presentation] ビタミンK を構造基盤とした抗腫瘍化合物の創製研究 (2021)
  • Author(s): 藤井晋也
  • Organizer: 日本ビタミン学会第73回大会
  • Invited
• [Presentation] 疎水性構造としてフェロセンを用いたアンドロゲン受容体リガンドの創製． (2021)
  • Author(s): 落合幸太郎，影近弘之，藤井晋也．
  • Organizer: 日本ケミカルバイオロジー学会第15回年会
• [Presentation] ケイ素官能基を用いたサブタイプ選択的LXRリガンドの創製研究． (2021)
  • Author(s): 難波奈央，松本雄一朗，橋本祐一，谷内出友美，影近弘之，藤井晋也．
  • Organizer: 日本ケミカルバイオロジー学会第15回年会
• [Presentation] アンドロゲン受容体リガンドを指向した二置換フェロセン誘導体の設計・合成と構造活性相関． (2021)
  • Author(s): 落合幸太郎，影近弘之，藤井晋也．
  • Organizer: 第47回反応と合成の進歩シンポジウム
• [Presentation] サブタイプ選択的LXRリガンドを指向したケイ素化合物の構造展開． (2021)
  • Author(s): 難波奈央，松本雄一朗，橋本祐一，谷内出友美，影近弘之，藤井晋也．
  • Organizer: 日本レチノイド研究会第32回学術集会
• [Presentation] 疎水性構造としてフェロセンを有する新規ARアンタゴニストの創製 (2021)
  • Author(s): 落合幸太郎，影近弘之，藤井晋也．
  • Organizer: 日本レチノイド研究会第32回学術集会
• [Presentation] 非汎用元素を用いた生物活性化合物の分子設計戦略 (2021)
  • Author(s): 藤井晋也
  • Organizer: 日本薬学会第141年会
• [Presentation] フェロセンを疎水性ファーマコフォアとする核内受容体リガンドの創製 (2021)
  • Author(s): 落合幸太郎，影近弘之，藤井晋也
  • Organizer: 日本薬学会第141年会
• [Presentation] N-メチル-N,N'-ジフェニルスクアルアミドの立体特性 (2021)
  • Author(s): 田中希実子，神田翠，藤井晋也，影近弘之，棚谷綾
  • Organizer: 日本薬学会第141年会
• [Presentation] ケイ素官能基を利用したレチノイドの疎水性部位の構造展開 (2020)
  • Author(s): 及川剛志，藤井晋也，増野弘幸，河内恵美子，森修一，影近弘之
  • Organizer: 日本ビタミン学会第72回大会
• [Presentation] シリル基を利用したレチノイド誘導体の疎水性部位に関する構造活性相関 (2020)
  • Author(s): 藤井晋也，及川 剛志，増野弘幸，河内恵美子，森修一，影近弘之
  • Organizer: 日本レチノイド研究会第31回学術集会
• [Presentation] ベンゼンスルホンアミドを基盤とした非ステロイド型プロゲステロン受容体リガンドの構造展開 (2020)
  • Author(s): 大谷和暉、山田歩、森修一、藤井晋也、影近弘之
  • Organizer: 日本薬学会第 140年会
• [Presentation] Boron cluster-based development of novel nuclear receptor modulators (2019)
  • Author(s): Shinya Fujii
  • Organizer: ICPAC2019 Yangon
  • Int'l Joint Research / Invited
• [Presentation] Phosphorus functionalities as novel options for structural development - Properties and estrogenic activity of 4-phosphinophenol derivatives - (2019)
  • Author(s): Hiroki Saito, Yuichiro Matsumoto, Hiroyuki Kagechika, Yuichi Hashimoto, Shinya Fujii
  • Organizer: ASMC 2019
  • Int'l Joint Research
• [Presentation] Development of novel silicon-containing transcription modulators including sila-heterocyclic compounds (2019)
  • Author(s): Hirozumi Toyama, Daisuke Kajita, Yuichi Hashimoto, Shinya Fujii
  • Organizer: BioHeterocycles 2019
  • Int'l Joint Research
• [Presentation] 多元素有機化合物の特性を活用した生物活性化合物の創製研究 (2019)
  • Author(s): 藤井晋也
  • Organizer: 第45回反応と合成の進歩シンポジウム
  • Invited
• [Presentation] リン原子の創出する構造多様性に着目した生物活性化合物の創製研究－ホスフィノフェノール誘導体の構造物性相関とERリガンド活性－ (2019)
  • Author(s): 齊藤広樹、 松本雄一朗、 橋本祐一、 藤井晋也
  • Organizer: 日本ケミカルバイオロジー学会 第14回年会
• [Presentation] ジフェニルホスフィン構造を基盤とした含リン化合物の性質の解明と医薬品構造要素としての有用性の検討 (2019)
  • Author(s): 齊藤広樹、 松本雄一朗 、 橋本祐一 、 影近弘之、藤井晋也
  • Organizer: 第37回メディシナルケミストリーシンポジウム
• [Presentation] 脂溶性ビタミンをリードとした創薬化学研究～新規骨格構造を有するビタミン誘導体の創製と生物活性～ (2019)
  • Author(s): 藤井晋也、影近弘之
  • Organizer: 第363回脂溶性ビタミン総合研究委員会
• [Presentation] 抗腫瘍活性を有するフタラジンジオン誘導体の創製 (2019)
  • Author(s): 内藤加菜、及川剛志、藤井晋也、 秦咸陽、小嶋聡一、影近弘之
  • Organizer: 日本レチノイド研究会第30回学術集会
• [Presentation] アンドロゲン合成酵素を標的とした新規去勢抵抗性前立腺がん治療薬の開発 (2019)
  • Author(s): 遠藤智史、瀬川仁、小栗弘成、夏爽、胡大イ、入江克雅、藤井晋也、合田浩明、松川卓生、藤本直浩、中山敏幸、豊岡尚樹、松永俊之、五十里彰
  • Organizer: 第47回構造活性相関シンポジウム
• [Presentation] Silyl groups as fancy isosteres of cis-diatomic functionalities ―Development of novel nuclear receptor modulators based on silyl functionalities－ (2018)
  • Author(s): 〇Shinya Fujii, Hirozumi Toyama, Daisuke Kajita, Yuichi Hashimoto
  • Organizer: RICT2018
  • Int'l Joint Research
• [Presentation] Structure-property and structure-activity relationships of heteroatom (Si, P, S)-containing bisphenols (2018)
  • Author(s): Yuichiro Matsumoto, Hiroki Saito, Yuichi Hashimoto, 〇Shinya Fujii
  • Organizer: ICPC22
  • Int'l Joint Research
• [Presentation] Silanol as a characteristic hydrophilic pharmacophore - Altered activity profile of a silanol analogue of multi-targeting nuclear receptor modulator T0901317 - (2018)
  • Author(s): 〇Shinya Fujii, Hirozumi Toyama, Yuichi Hashimoto
  • Organizer: EFMC-ISMC 2018
  • Int'l Joint Research
• [Presentation] レチノイド標的遺伝子のゲノムワイドな解析を指向したChem-seqプローブの創製研究 (2018)
  • Author(s): 〇藤井晋也，森修一，影近弘之，Marco Antonio Mendoza Parra，Hinrich Gronemeyer
  • Organizer: 日本ケミカルバイオロジー学会第13回年会
• [Presentation] 核内受容体リガンドの疎水性構造の研究～ケイ素含有化合物の構造展開～ (2018)
  • Author(s): 〇藤井晋也、橋本祐一、影近弘之
  • Organizer: 第359回脂溶性ビタミン総合研究委員会
• [Presentation] 創薬化学における高周期元素の利用法の検討種々の元素をリンカー構造に有するビスフェノール誘導体の構造物性相関および構造活性相関 (2018)
  • Author(s): 〇松本雄一朗, 橋本祐一, 藤井晋也
  • Organizer: 日本レチノイド研究会第29回学術集会
• [Presentation] ケイ素官能基をリンカー構造とするビスフェノール誘導体の構造物性相関と選択的エストロゲン受容体モジュレータへの展開 (2018)
  • Author(s): 〇松本雄一朗, 橋本祐一, 藤井晋也
  • Organizer: 第36回メディシナルケミストリーシンポジウム
• [Presentation] ホスフィノフェノール構造を基盤とする含リン化合物の構造物性相関と生物活性化合物への応用 (2018)
  • Author(s): 〇齊藤広樹、 松本雄一朗、 橋本祐一、 藤井晋也
  • Organizer: 第36回メディシナルケミストリーシンポジウム
• [Presentation] Development of chemical probes designed for genome-wide analysis of retinoid targets (2018)
  • Author(s): Fujii, S.; Mori, S.; Kagechika, H.; Mendpza Parra, M. A.; Gronemeyer, H.
  • Organizer: JSPS Core-to-core Program Symposium
  • Int'l Joint Research
• [Presentation] ビスフェノール構造を基盤としたケイ素官能基の構造物性および構造活性相関 (2018)
  • Author(s): 松本雄一朗、橋本祐一、藤井晋也
  • Organizer: 日本薬学会第138年会
• [Presentation] ビタミンD活性を有するカルボラン含有カルボン酸誘導体 (2018)
  • Author(s): 塚本理穂、増野弘幸、藤井晋也、河内恵美子、影近弘之
  • Organizer: 日本薬学会第138年会
• [Presentation] Application of Boron Clusters in Medicinal Chemistry (2017)
  • Author(s): Fujii, S.
  • Organizer: 17th International Conference on Heterocycles in Bioorganic Chemistry
  • Int'l Joint Research
• [Presentation] レチノイド標的遺伝子のゲノムワイドな探索を指向した低分子プローブの創製研 (2017)
  • Author(s): 藤井晋也，森修一，影近弘之, Marco Antonio Mendoza Parra, Hinrich Gronemeyer
  • Organizer: 日本レチノイド研究会第２８回学術集会
• [Presentation] Phenanthridin-6(5H)-one骨格を有する非ステロイド型プロゲステロン受容体拮抗薬の創製 (2017)
  • Author(s): 西山郵子、森修一、槇島誠、藤井晋也、影近弘之、橋本祐一、石川稔
  • Organizer: 日本レチノイド研究会第２８回学術集会
• [Presentation] 種々のケイ素含有置換基を有する新規レチノイドの創製 (2017)
  • Author(s): 及川剛志、藤井晋也、増野弘幸、河内恵美子、影近弘之
  • Organizer: 第35回メディシナルケミストリーシンポジウム
• [Presentation] m-カルボランを疎水性骨格とした新規プロゲステロン受容体リガンドの創製 (2017)
  • Author(s): 森修一、高垣亮平、藤井晋也、棚谷綾、影近弘之
  • Organizer: 第35回メディシナルケミストリーシンポジウム