2. Academic Validation
  3. Synthesis of 1-O-acyl- and 1-oxo-kamebanin analogues and their cytotoxic activity

Synthesis of 1-O-acyl- and 1-oxo-kamebanin analogues and their cytotoxic activity

  • Bioorg Med Chem Lett. 2023 Feb 15:82:129149. doi: 10.1016/j.bmcl.2023.129149.
Yutaka Aoyagi 1,  Kaori Tomita 2,  Asumi Kobayashi 2,  Akari Nakamura 2,  Yuki Fujii 2,  Momoka Yagi 2,  Yoshimi Ichimaru 2,  Kei Ozawa 3,  Hyun-Sun Park 3,  Haruhiko Fukaya 3,  Reiko Yano 2,  Tomoyo Hasuda 3,  Koichi Takeya 3,  Yukio Hitotsuyanagi 4,  Ming-Yu Gui 5,  Yong-Ri Jin 5,  Xu-Wen Li 5
Affiliations

Affiliations

  • 1 College of Pharmacy, Kinjo Gakuin University, 2-1723 Omori, Moriyama-ku, Nagoya, Aich 463-8521, Japan. Electronic address: [email protected].
  • 2 College of Pharmacy, Kinjo Gakuin University, 2-1723 Omori, Moriyama-ku, Nagoya, Aich 463-8521, Japan.
  • 3 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
  • 4 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan. Electronic address: [email protected].
  • 5 Department of Chemistry, JiLin University, No. 2 Xinmin street, Changchun, JiLin 130021, China.
PMID: 36690039 DOI: 10.1016/j.bmcl.2023.129149
Abstract

A series of 1-O-acyl- and 1-oxo-kamebanin analogues were prepared from kamebanin, isolated from Rabdosia excisa and their cytotoxicity was assayed on HL60 promyelocytic leukemia cells and HCT116 human colon Cancer cells. The structure-activity relationship study showed that the presence of 1-O-acyl groups of a C3-C5 carbon chain increased the cytotoxic activity.

Keywords

Cytotoxicity; Ent-kaurene; Kamebanin; Semi-synthesis; Structure–activity relationship.

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