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Synthetic Organic Chemistry for Drug Development(Chemistry)

Nakayama AtsushiAssociate professor

Born in Tama City, Tokyo. Graduated from the Faculty of Pharmaceutical Sciences, Chiba University in 2007. Completed the Doctoral Program at the Graduate School of Pharmaceutical Sciences, Chiba University in 2012 (Ph.D. in Pharmacy under the supervision of Prof. Hiromitsu Takayama). From 2012, Postdoctoral Research Fellow at the Scripps Research Institute, USA (under Prof. Dale L. Boger). In 2014, became an Assistant Professor at the Faculty of Pharmaceutical Sciences, Tokushima University (under Prof. Kosuke Namba). In 2020, appointed as a Lecturer at the Faculty of Science, Osaka City University (currently Osaka Metropolitan University, under Prof. Tetsuro Shinada). Starting from July 2024, holds current position.

Research theme

Total Synthetic Study of Bioactive Natural Products

Since ancient times, mankind has sought molecules from nature to regulate biological phenomena, using these natural products either as medicines themselves or as seed compounds for drug development. However, the complex structures of natural products make their construction challenging, and as a result many natural products with potential value remain unexplored. Our research focuses on the development of synthetic strategies and new methodologies for the efficient synthesis of natural products through organic chemistry. By providing promising bioactive natural products, we aim to explore their potential as therapeutic agents.

Medicinal Chemistry of “Pseudo-Natural Products”

The biological activities of natural products have often been refined through evolution, but they do not necessarily represent a "final form". Our research focuses on the molecular scaffolds of natural products, specifically modifying those scaffold regions that are difficult or impossible to modify by biosynthesis. We chemically engineer these structurally modified compounds, known as “pseudo-natural products”, to explore their potential value. As scaffold modification requires the total synthesis of the target molecules, we conduct pseudo-natural product synthesis research in parallel with the synthesis of bioactive natural products.

Representative achievements

Studies on Comprehensive Total Synthesis of Natural and Pseudo-Natural Products for Drug Discovery
Atsushi Nakayama
Chemical and Pharmaceutical Bulletin, 72, 422-431 (2024)

Total Synthesis of Bipenicilisorin and Assignment of the Absolute Configuration
Eigo Fukuda, Ibuki Fujiwara, Shoki Maruno, Kaiki Motomura, Seiya Endo, Arihiro Iwasaki, Tatsuya Fukuta, Atsushi Nakayama*, Tetsuro Shinada*
Journal of Natural Products, 87, 1394-1400 (2024)

Therapeutic efficacy of the resorcylic acid lactone LL‐Z1640‐2 for adult T‐cell leukaemia/lymphoma
Masahiro Oura, Takeshi Harada*, Asuka Oda, Jumpei Teramachi, Atsushi Nakayama, Ryohei Sumitani, Yusuke Inoue, Yusaku Maeda, Kimiko Sogabe, Tomoko Maruhashi, Mamiko Takahashi, Shiro Fujii, Shingen Nakamura, Hirokazu Miki, Masafumi Nakamura, Tomoyo Hara, Hiroki Yamagami, Kiyoe Kurahashi, Itsuro Endo, Hiroo Hasegawa, Hiroshi Fujiwara, Masahiro Abe*
eJHaem, 4, 667–678 (2023)

Concise Synthesis of Isocoumarin-3-carboxylic Acid Esters
Atsushi Nakayama*, Kenichiro Hamamoto†, Ibuki Fujiwara†, Eigo Fukuda, Keita Ozawa, Seiya Endo, Rika Yamasaki, Hidemitsu Yamanaka, Yusaku Tamura, Yuki Yamamoto, Tetsuro Shinada*
Chemistry Letters, 52, 640–643 (2023)

Synthesis of Drimane-8α,11-diol Using Terpene Cyclase from Bacillus megaterium
Keita Ozawa, Yuki Yamamoto, Eigo Fukuda, Seiya Endo, Atsushi Nakayama, Yoko Yasuno, Daijiro Ueda, Tsutomu Sato, Tetsuro Shinada*
Chemistry Letters, 52, 520–523 (2023)

1,3a,6a-Triazapentalene derivatives as photo-induced cytotoxic small fluorescent dyes
Daisuke Tsuji*, Atsushi Nakayama, Riko Yamamoto, Shuji Nagano, Takashi Taniguchi, Ryota Sato, Sangita Karanjit, Naoki Muguruma, Tetsuji Takayama, Kohji Itoh, Kosuke Namba*
Communications Chemistry, 6, Article No. 37 (2023)

Stereoselective Syntheses of trans-Anhydromevalonic Acid and trans-Anhydromevalonyl Group-Containing Natural Products
Atsushi Nakayama, Yoko Yasuno, Yuki Yamamoto, Kai Saito, Kohei Kitsuwa, Hironori Okamura, Tetsuro Shinada*
Journal of Natural Products, 85, 1052–1058 (2022)

Concise Total Synthesis of Tronocarpine
Atsushi Nakayama*, Tenta Nakamura, Toshihiro Zaima, Saho Fujimoto, Sangita Karanjit, Kosuke Namba*
Angewandte Chemie International Edition, 60, 635–639 (2021)

Development of a 1,3a,6a-triazapentalene derivative as a compact and thiol-specific fluorescent labeling reagent
Atsushi Nakayama, Akira Otani, Tsubasa Inokuma, Daisuke Tsuji, Haruka Mukaiyama, Akira Nakayama, Kohji Itoh, Akira Otaka, Keiji Tanino, Kosuke Namba*
Communications Chemistry, 3, Article No.6 (2020)

Total Syntheses and Initial Evaluation of [Psi[C(=S)NH]Tpg(4)]vancomycin, [Psi[C(=NH)NH]Tpg(4)]vancomycin, [Psi[CH2NH]Tpg(4)]vancomycin, and Their (4-Chlorobiphenyl)methyl Derivatives: Synergistic Binding Pocket and Peripheral Modifications for the Glycopeptide Antibiotics
Akinori Okano, Atsushi Nakayama, Kejia Wu, Erick A. Lindsey, Alex W. Schammel, Yiqing Feng, Karen C. Collins, Dale L. Boger*
Journal of the American Chemical Society, 137, 3693–3704 (2015)