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Light-promoted stereoselective late-stage difunctionalization and anti-tumor activity of oridonin.
Tang, Qianhui; Lu, Yougan; Song, Junying; He, Zhengyang; Xu, Jin-Bu; Tan, Jiao; Gao, Feng; Li, Xiaohuan.
Afiliación
  • Tang Q; School of Life Science and Engineering, Southwest Jiaotong University, No. 111, Erhuan Rd, Chengdu 610031, PR China.
  • Lu Y; School of Life Science and Engineering, Southwest Jiaotong University, No. 111, Erhuan Rd, Chengdu 610031, PR China.
  • Song J; School of Life Science and Engineering, Southwest Jiaotong University, No. 111, Erhuan Rd, Chengdu 610031, PR China.
  • He Z; School of Life Science and Engineering, Southwest Jiaotong University, No. 111, Erhuan Rd, Chengdu 610031, PR China.
  • Xu JB; School of Life Science and Engineering, Southwest Jiaotong University, No. 111, Erhuan Rd, Chengdu 610031, PR China.
  • Tan J; School of Pharmacy, Chongqing Medical and Pharmaceutical College, No.82, University Town Central Road, Chongqing 401331, PR China.
  • Gao F; School of Life Science and Engineering, Southwest Jiaotong University, No. 111, Erhuan Rd, Chengdu 610031, PR China.
  • Li X; School of Life Science and Engineering, Southwest Jiaotong University, No. 111, Erhuan Rd, Chengdu 610031, PR China. Electronic address: xiaohuanli@swjtu.edu.cn.
Fitoterapia ; 177: 106131, 2024 Sep.
Article en En | MEDLINE | ID: mdl-39067489
ABSTRACT
The late-stage difunctionalization of diterpene oridonin by light-promoted direct oxyamination with various O-benzoylhydroxylamines was carried out to afford C16α-N-C17-OBz-oridonin derivatives (1-25) for the first time. Though as a radical reaction, it features high stereoselectivity to only produce C16α-N-C17-OBz-oridonins. The in vitro antiproliferative activity of these C16α-N-C17-OBz-oridonins against the human breast cancer cell lines (MCF-7) was evaluated by MTT assay, showing that most of the synthesized compounds possessed moderate anticancer activity against MCF-7 cell lines superior or similar to the parent compound oridonin. The derivative 25 with a N-methyl-N-(naphthalen-1-ylmethyl) substitution showed better cytotoxicity against MCF-7 cells (IC50 value of 11.75 µM) than oridonin (IC50 value of 17.95 µM).
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diterpenos de Tipo Kaurano / Antineoplásicos Fitogénicos Límite: Humans Idioma: En Revista: Fitoterapia Año: 2024 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diterpenos de Tipo Kaurano / Antineoplásicos Fitogénicos Límite: Humans Idioma: En Revista: Fitoterapia Año: 2024 Tipo del documento: Article Pais de publicación: Países Bajos