教員紹介

SDGsへの取り組み

最終学歴

九州大学大学院薬学研究科修士課程修了（製薬化学専攻）

取得学位

薬学博士（京都大学）

所属学会

日本薬学会、有機合成化学協会

現在の専門分野

有機化学、生物有機化学、医薬化学

現在の研究課題

●スイッチング反応の解明と制御
●Gタンパク質共役型受容体の活性制御分子の創生
●抗腫瘍活性物質の創生

主要研究業績

●分子内Diels-Alder反応の反応制御機構の解明
●プロスタグランジン受容体活性化におけるスイッチング反応の解明
●抗腫瘍活性を有する非麻薬性オピオイド類の創生
●新規DNAインターカレーターの創生

最近の研究業績

1. Yoshiko Furukawa, Y.; Sawamoto, A.; Yamaoka, M.; Nakaya, M.; Hieda, Y.; Choshi, T.; Hatae, N.; Okuyama, S.; Nakajima, M.; Hibino, S. Effects of Carbazole Derivatives on Neurite Outgrowth and Hydrogen Peroxide-Induced Cytotoxicity in Neuro2a Cells. Molecules, inpress (2019).

2. Nishiyama, T.; Hatae, N.; Chikaraishi, K.; Uchida, K.; Yokoyama, C.; Hibino, S.; Choshi. T. Concise Synthesis of Kalasinamide, Marcanine A, and Geovanine, and Antiproliferative Activity Evaluation of Their Azaanthracenones. Heterocycles, inpress (2018).

3. Stewart, N. J.; Kumeta, H.; Tomohiro, M.; Hashimoto, T; Hatae, N.; Matsumoto, S. Long-range heteronuclear J-coupling constants in esters: Implications for 13C metabolic MRI by side-arm parahydrogen-induced polarization. J. Magn. Reson., 296, 85-92 (2018).

4. Nishiyama, T.; Fujiwaki, T.; Hatae, N.; Uchiyama, E.; Takeuchi, N.; Minami, K.; Ishikura, M.; Hibino, S.; Choshi, T. Concise Synthesis of Azafluorenone and Its Application to Indeno[1,2-c]Isoquinolone. Heterocycles, 97, 383-394 (2018).

5. Hatae, N.; Kujime, E.; Yano, K.; Kizuka, M.; Ashida, R.; Choshi, T.; Nishiyama, T.; Okada, C.; Iwamura, T.; Yoshimura, T. Synthesis of N-ω-Phenylalkyl-4-(p-Chlorophenyl)-Piperidin-4-ol Analogues with Potent Antiproliferative Activity Against HCT-116 Cells. Heterocycles, 97, 560-568 (2018).

6. Nishiyama, T.; Hironaka, M.; Taketomi, M.; Taguchi, E.; Kotouge, R.; Shigemori, Y.; Hatae, N.; Ishikura, M.; Choshi, T. Total Synthesis of Two 8-Oxoprotoberberine Alkaloids: Alangiumkaloids A and B. Eur. J. Org. Chem., 673-678 (2018).

7. Itoh, T.; Hatae, N.; Nishiyama, T.; Choshi, T.; Hibino, S.; Yoshimura, T.; Ishikura, M. Synthesis and cytotoxicity of pyrido[4,3-b]carbazole alkaloids against HCT-116 and HL-60 cells. Med. Chem. Res., 27, 412-419 (2018).

8. Nishiyama, T.; Hatae, N.; Mizutani, M.; Yoshimura, T.; Kitamura, T.; Miyano, M.; Fujii, M.; Satsuki, N.; Ishikura, M.; Hibino, S.; Choshi, T. Concise synthesis and antiproliferative activity evaluation of ellipticine quinone and its analogs. Eur. J. Med. Chem., 136, 1-13 (2017).

9. Kobayashi, Y.; Tanahashi, R.; Yamaguchi, Y.; Hatae, N.; Kobayashi, M.; Ueno, Y.; Yoshimatsu, M. Ni-Pd Catalyzed Cyclization of Sulfanyl 1,6-Diynes: Synthesis of 1’-Homonucleoside Analogues. J. Org. Chem., 82, 2436-2449 (2017).

10. Hatae, N.; Sakai, Y.; Yorozu, K.; Okada, C.; Yoshimatsu, M.; Yoshimura, T. Synthesis of -dihydropyrrolyl and -pyrrolyl acrylates and their antiproliferative activity against HCT-116 and HL-60 cells. Heterocycles, 95, 557-567 (2017).

11. Nishiyama, T.; Hatae, N.; Hayashi, K.; Obata, M.; Taninaka, K.; Yamane, M.; Oda, S.; Abe T.; Ishikura, M.; Hibino, S.; Choshi, T. One-pot synthesis of fused 2-pyridones from heteroarylacrylic acid via Curtius rearrangement and microwave-assisted thermal electrocyclization. Heterocycles, 95, 251-267 (2017).

12. Nishiyama, T.; Hatae, N.; Yoshimura, T.; Takaki, S.; Abe, T.; Ishikura, M.; Hibino, S.; Choshi, T. Concise synthesis of carbazole-1,4-quinones and evaluation of their antiproliferative activity against HCT-116 and HL-60 cells. Eur. J. Med. Chem., 121, 561-577 (2016).

13. Hatae, N.; Nishiyama, T.; Tamura, S.; Yamamoto, R.; Matsui, A.; Shinchi, H.; Hibino, S.; Okada, C.; Yoshimura, T.; Choshi, T.; Toyota, E. Antiproliferative activity of hybrid compounds between 6-methoxy-3-(4-methoxyphenyl)-1H-indole and 4-phenylpiperidine against HCT-116 and HL-60 cells. Heterocycles, 93, 440-452 (2016).

14. Hieda, Y.; Hatae, N.; Anraku, M.; Matsuura, N.; Uemura, K.; Hibino, S.; Choshi, T.; Tomida, H.; Hori, O.; Fujioka, H. Antioxidant effects of the hydroxyl groups in the simple phenolic carbazoles. Heterocycles, 92, 120-132 (2016).

15. Yoshimatsu, M.; Tanaka, M.; Fujimura, Y.; Ito, Y.; Goto, Y.; Kobayashi, Y.; Wasada, H.; Hatae, N.; Tanabe, G.; Muraoka, O. Synthesis of Azepines via a [6+1] Annulation of Ynenitriles with Reformatsky Reagents. J. Org. Chem., 80, 9480-9494 (2015).

16. Hatae, N.; Fujita, E.; Shigenobu, S.; Shimoyama, S.; Ishihara, Y.; Kurata, Y.; Choshi, T.; Nishiyama, T.; Okada, C.; Hibino, S. Antiproliferative activity of O4-benzo[c] phenanthridine alkaloids against HCT-116 and HL-60 tumor cells. Bioorg. Med. Chem. Lett., 25, 2749-2752 (2015).

17. Choshi, T.; Hironaka, M.; Goto, M.; Shimizu, K.; Kurata, Y.; Nishiyama, T.; Hatae, N.; Hibino, S. NOVEL TOTAL SYNTHESIS OF THE 2-AZAANTHRAQUINONE ALKALOID SCORPINONE USING A TANDEM OXIDATION AND AZAELECTROCYCLIC REACTION. Heterocycles, 91, 537-549 (2015).

18. Hatae, N.; Kaji, A.; Okada, C.; Toyota, E. TANDEM [4+2] CYCLOADDITION/AROMATIZATION SEQUENCE OF ALLENYL 2-BROMO-3-VINYLCYCLOHEX-2-ENYL THIOETHER TO NAPHTO[1,8-bc]THIOPHENE. Heterocycles, 90, 157-162 (2015).

19. Hatae, N.; Suzuki, I.; Choshi, T.; Hibino, S.; Okada, C.; Toyota, E. Halogen effect on tandem [4+2] cycloaddition/aromatization sequence of allenyl 2-halo-3-vinylcyclohex-2-enyl ether. Tetrahedron Lett., 55, 4146-4148 (2014).

20. Hatae, N.; Satoh, R.; Chiba, H.; Osaki, T.; Nishiyama, T.; Ishikura, M.; Abe, T.; Hibino, S.; Choshi, T.; Okada, C.; Toyota, E. N-Substituted calothrixin B derivatives inhibited the proliferation of HL-60 promyelocytic leukemia cells. Med. Chem. Res., 23, 4956-4961 (2014).

21. Hieda, Y.; Anraku, M.; Choshi, T.; Tomida, H.; Fujioka, H.; Hatae, N.; Hori, O.; Hirose, J.; Hibino, S. Antioxidant effects of the highly-substituted carbazole alkaloids and their related carbazoles. Bioorg. Med. Chem. Lett., 24, 3530-3533 (2014).

22. Hatae, N.; Yamauchi, S.; Saeki, T.; Suzuki, I.; Choshi, T.; Hibino, S.; Okada, C.; Hayashi, M.; Watanabe, Y.; Toyota, E. Effects of 1,3-di-O-substituted myo-inositol derivatives on the antiproliferation and caspase-3 activation of HCT-116 and HL-60 cells. Chem. Biol. Lett., 1, 40-43 (2014).

23. Tazaki, Y.; Tsuchiya, Y.; Choshi, T.; Nishiyama, T.; Hatae, N.; Nemoto, H.; Hibino, S. The First Total Synthesis of the Antiplasmodial Alkaloid (±)-Cassiarin C Based on a Microwave-Assisted Thermal Azaelectrocyclic Reaction. Heterocycles, 89, 427-435 (2014).

24. Hatae, N.; Nagayama, T.; Esaki, H.; Kujime, E.; Minami, M.; Ishikura, M.; Choshi, T.; Hibino, S.; Okada, C.; Toyota, E.; Nagasawa, H.; Iwamura, T. Synthesis of 4-Arylpiperidin-4-ol Derivatives of Loperamide as Agents with Potent Antiproliferative Effects against HCT-116 and HL-60 Cells. Heterocycles, 88, 663-673 (2014).

25. Kurata, Y.; Choshi, T.; Ishihara, Y.; Hatae, N.; Nishiyama, T.; Hibino, S. Total Synthesis of the Benzo[c]phenanthridine Alkaloids, Terihanine and Isoterihanine, and Their Antitumor Activity. Heterocycles, 88, 297-308 (2014).

26. Abe, T.; Ikeda, T.; Itoh, T.; Hatae, N.; Toyota, E.; Ishikura, M. One-Pot Access to 3,3’-Bisindolylmethanes through the Intermolecular Pummerer Reaction. Heterocycles, 88, 187-191 (2014).

27. Hatae, N.; Nakamura, J.; Okujima, T.; Ishikura, M.; Abe, T.; Hibino, S.; Choshi, T.; Okada, C.; Yamada, H.; Uno, H.; Toyota, E. Effect of the orthoquinone moiety in 9,10-phenanthrenequinone on its ability to induce apoptosis in HCT-116 and HL-60 cells. Bioorg. Med. Chem. Lett., 23, 4637-4640 (2013).

28. Tagawa, S.; Choshi, T.; Okamoto, A.; Nishiyama, T.; Watanabe, S.; Hatae, N.; Ishikura, M.; Hibino, S. Enantioselective total synthesis of 1,3-disubstituted -carboline alkaloids, (-)-Dichotomine A and (+)-Dichotomide II. Eur. J. Org. Chem., 1805-1810 (2013).

29. Tagawa, S.; Choshi, T.; Okamoto, A.; Nishiyama, T.; Watanabe, S.; Hatae, N.; Hibino, S. FIRST TOTAL SYNTHESES OF 1,3-DISUBSTITUTED -CARBOLINE ALKALOIDS, DICHOTOMIDE I AND MARINACARBOLINES A-D. Heterocycles, 87, 357-367 (2013).

30. Abe, T.; Komatsu, H.; Ikeda, T.; Hatae, N.; Toyota, E.; Ishikura, M. Short approach to bisindole alkaloid, Yuehchukene, using 2-indolylcyanocuprate. Heterocycles, 86, 505-513 (2012).

31. Abe, T.; Ikeda, T.; Choshi, T.; Hibino, S.; Hatae, N.; Toyota, E.; Yanada, R.; Ishikura, M. Total Synthesis of Calothrixins A and B by Palladium-Catalyzed Tandem Cyclization/Cross-Coupling Reaction of Indolylborate. Eur. J. Org. Chem., 5018-5027 (2012).

32. Matsumoto, K.; Choshi, T.; Hourai, M.; Zamami, Y.; Sasaki, K.; Abe, T.; Ishikura, M.; Hatae, N.; Iwamura, T.; Tohyama, S.; Nobuhiro, J.; Hibino, S. Synthesis and Antimalarial Activity of Calothrixins A and B, and their N-Alkyl Derivatives. Bioorg. Med. Chem. Lett., 22, 4762-4764 (2012).

33. Hayashi, K.; Choshi, T.; Chikaraishi, K.; Oda, A.; Yoshinaga, R.; Hatae, N.; Ishikura, M.; Hibino, S. A novel total synthesis of isocryptolepine based on a microwave-assisted tandem Curtius rearrangement and aza-electrocyclic reaction. Tetrahedron, 68, 4274-4279 (2012).

34. Uno, H.; Fujimoto, A.; Furukawa, M.; Hatae, N.; Iwamura, T.; Komatsu, N.; Kuramoto, M.; Mori, S.; Okujima, T.; Tani, F.; Uoyama, H.; Watanabe, H.; Yamada, H. Porphyrin Molecular Tweezers for Fullerenes. J. Porphyrins Phthalocyanines, 15, 951-963 (2011).

35. Yamada, K.; Yamaguchi, S.; Hatae, N.; Abe, T.; Iwamura, T.; Ishikura, M. Facile synthesis of pyrano[3,2-e]indoles via the base-promoted Pictet-Spengler reaction of Nb-(benzyl)serotonin. Heterocycles, 83, 815-826 (2011).

36. Yamaoka, K.; Yano, A.; Kuroiwa, K.; Morimoto, K.; Inazumi, T.; Hatae, N.; Tabata, H.; Segi-Nishida, E.; Tanaka, S.; Ichikawa, A.; Sugimoto, Y.. Prostaglandin EP3 receptor superactivates adenylyl cyclase via the Gq/PLC/Ca2+ pathway in a lipid raft-dependent manner. Biochem. Biophys. Res. Commun., 389, 678-682 (2009).

37. Hatae, N.; Aksentijevich, N.; Zemkova, H. W.; Kretschmannova, K.; Tomic, M.; Stojilkovic, S. S. Cloning and functional identification of novel endothelin receptor type A isoforms in pituitary. Mol. Endocrinol., 21, 1192-1204 (2007).

■Research mapはこちら■

受賞

●日本薬学会近畿支部奨励賞
●ジュニアドベンチャー選手権愛媛信用金庫賞
●愛媛大学・松山大学連携事業報告会学長賞

著書及び総説

●「新編 医薬化学」（分担編集・分担著書）　廣川書店（2018年3月）
●「Rice Studies, Present and Future (2011)」（分担共著）　三共出版（2012年3月）
●「CBT対策と演習 医薬品化学」（分担共著）　廣川書店（2009年10月）
●「NEW医薬品化学」（分担共著）　廣川書店（2008年2月）
●「バイオインフォマティクス事典」（分担著書）　共立出版（2006年7月）