Yusuke Akagi
| Faculty of Pharmaceutical Sciences,Department of Pharmaceutical Sciences | Lecturer |
Last Updated :2025/10/07
■Researcher basic information
■Research activity information
Paper
- Side-Chain Fluorine Engineering of Vitamin D<sub>3</sub> Derivatives for VDR-Silent SREBP Inhibitors
Fumihiro Kawagoe; Sayuri Mototani; Tomofumi Yatsu; Yasushi Takemoto; Yusuke Akagi; Toshie Fujishima; Yoshiki Miyata; Motonari Uesugi; Atsushi Kittaka
Chemical and Pharmaceutical Bulletin, 20 Sep. 2025, [Reviewed] - Synthesis and in Vitro Cytotoxicity Evaluation of Jadomycins
Erika Iwasaki; Yoshimi Shimizu; Yusuke Akagi; Toshiya Komatsu
Chemical and Pharmaceutical Bulletin, 01 Sep. 2023, [Reviewed]
Jadomycins, which are benzo[b]phenanthridine-type alkaloids isolated from Streptomyces venezuelae ISP5230, exhibit cytotoxic activity against multidrug-resistant breast cancer cells. We have previously achieved the total synthesis of jadomycins using the direct arylation of juglone as a key step. In this study, we achieved the total synthesis of jadomycin T and jadomycin aglycons using L-threonine and 1-amino-2-propanol as nitrogen sources. Additionally, we evaluated the cytotoxic activity of eight compounds, including glycosides, jadomycin T, and their corresponding aglycons, in eight types of tumor cells. The evaluated jadomycins tended to exhibit stronger cytotoxic activity as aglycons than as glycosides. Although the presence of a 1,3-oxazolidine ring derived from an amino acid was not essential, the presence of the 1,3-oxazolidine ring showed strong activity when the ring had a carboxyl group. Furthermore, compared to the non-natural isomer at a different position on the phenolic hydroxyl group, the naturally occurring phenanthroviridin aglycon exhibited stronger cytotoxic activity. In addition, this study suggests that jadomycins may become lead compounds for the treatment of brain tumors; however, further studies on their ability to penetrate the blood-brain barrier are required. - Total synthesis of jadomycins A, B, and l-digitoxosyl-phenanthroviridin
Yusuke Akagi; Yuta Mori; Yudai Sato; Erika Iwasaki; Toshiya Komatsu
Tetrahedron Letters, Jul. 2022, [Reviewed] - Discovery of a Vitamin D Receptor-Silent Vitamin D Derivative That Impairs Sterol Regulatory Element-Binding Protein In Vivo
Fumihiro Kawagoe; Aileen Mendoza; Yuki Hayata; Lisa Asano; Kenjiro Kotake; Sayuri Mototani; Satoshi Kawamura; Shigeyuki Kurosaki; Yusuke Akagi; Yasushi Takemoto; Kazuo Nagasawa; Hayato Nakagawa; Motonari Uesugi; Atsushi Kittaka
Journal of Medicinal Chemistry, 13 May 2021, [Reviewed] - Total Synthesis of Phenanthroviridin Aglycon and Its Analog
Yusuke Akagi; Kohei Harasawa; Toshiya Komatsu
Asian Journal of Organic Chemistry, May 2021, [Reviewed] - Palladium-catalyzed arylation of 1,4-naphthoquinones with aryl iodides and its synthetic application to the benzo[b]phenanthridine skeleton
Akagi, Y.; Komatsu, T.
Tetrahedron Letters, 2020, [Reviewed] - Palladium-Catalyzed β-Arylation of Cyclic α,β-Unsaturated O-Methyl Oximes with Aryl Iodides
Akagi, Y.; Fukuyama, S.; Komatsu, T.
Chemical & pharmaceutical bulletin, 2020, [Reviewed] - Synthetic Chemical Probes That Dissect Vitamin D Activities
Nagata, A.; Akagi, Y.; Asano, L.; Kotake, K.; Kawagoe, F.; Mendoza, A.; Masoud, S.S.; Usuda, K.; Yasui, K.; Takemoto, Y.; Kittaka, A.; Nagasawa, K.; Uesugi, M.
ACS Chemical Biology, 2019, [Reviewed] - Stereoselective Synthesis of Four Calcitriol Lactone Diastereomers at C23 and C25
Nagata, A.; Akagi, Y.; Masoud, S.S.; Yamanaka, M.; Kittaka, A.; Uesugi, M.; Odagi, M.; Nagasawa, K.
Journal of Organic Chemistry, 2019, [Reviewed] - Synthetic studies of (23S,25R)-1α,25-dihydroxyvitamin D
3 26,23-lactone (calcitriol lactone) and its derivatives
Akagi, Y.; Nagata, A.; Odagi, M.; Nagasawa, K.
Journal of Steroid Biochemistry and Molecular Biology, 2018, [Reviewed] - A-Ring Synthons of 19-Nor Type Vitamin D Derivatives
Akagi, Y.; Yasui, K.; Nagasawa, K.
Journal of Steroid Biochemistry and Molecular Biology, 2017, [Reviewed] - Synthesis of diastereomers of 1,3-cis-25-dihydroxy-19-norvitamin D
3
Usuda, K.; Biswas, T.; Yamaguchi, T.; Akagi, Y.; Yasui, K.; Uesugi, M.; Shimizu, I.; Hosokawa, S.; Nagasawa, K.
Chemical and Pharmaceutical Bulletin, 2016, [Reviewed] - Synthesis of 24,24-difluoro-1,3-cis-25-dihydroxy-19-norvitamin D
3 derivatives and evaluation of their vitamin D receptor-binding affinity
Biswas, T.; Akagi, Y.; Usuda, K.; Yasui, K.; Shimizu, I.; Okamoto, M.; Uesugi, M.; Hosokawa, S.; Nagasawa, K.
Biological and Pharmaceutical Bulletin, 2016, [Reviewed] - Synthesis of 1 α- and 1 β-amino-25-hydroxyvitamin D
3
Akagi, Y.; Usuda, K.; Tanami, T.; Yasui, K.; Asano, L.; Uesugi, M.; Nagasawa, K.
Asian Journal of Organic Chemistry, 2016, [Reviewed] - Synthesis of jadomycin A and related jadomycin aglycons: Structural re-examination of jadomycins S and T may be needed
Tajima, T.; Akagi, Y.; Kumamoto, T.; Suzuki, N.; Ishikawa, T.
Tetrahedron Letters, 2012, [Reviewed] - Synthetic studies on jadomycins: synthesis of dimethyljadomycin A
Akagi, Y.; Yamada, S.-i.; Etomi, N.; Kumamoto, T.; Nakanishi, W.; Ishikawa, T.
Tetrahedron Letters, 2010, [Reviewed]
Research Themes
- 天然物合成を指向したナフトキノンの位置選択的なアリール化反応の開発とその応用
01 Apr. 2025 - 31 Mar. 2028
