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Synthesis and in vitro Anti-proliferative Activities on LNCaP, LS180 and MKN45 of Novel 20(R)-Panaxadiol Derivatives by Jianqiang Deng; Xinyu Yang; Mingzhu Luan; Shuqi Liu; Juan Zhang; Sheng Jiang; Wenshui Wang; Guige Hou; Qingguo Meng; Hongbo Wang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Background: 20(R)-PD, a tetracyclic triterpenoid, is a non-natural saponin present in the form of protopanaxadiol. Because of its essential biological activities, especially anti-tumor activity, structural modification of 20(R)-PD and the development of innovative and novel 20(R)-PD derivatives with better anti-tumor activity are increasingly relevant. ## Aims: 20(R)-Panaxadiol (20(R)-PD) can inhibit tumor proliferation. Three series of novel 20(R)-PD derivatives were synthesized by modifying the A-ring. ## Objective: The objective of this work was to synthesize and evaluate the in vitro anti-proliferative activities of 20(R)- PD derivatives in LNCaP, LS180, and MKN45 cancer cells. Structural modifications were performed at the C-3 position and A-ring. ## Methods: The in vitro anti-proliferative activities of novel derivatives in LNCaP, LS180, and MKN45 cells were evaluated by the MTT assay. The effects of compounds 5 and C9 on apoptosis were determined by flow cytometry. ## Results: Compounds 5, B2, C2, C4, C7, C8, C9, C10, and C11 exhibited good anti-proliferative activities in LNCaP, LS180, and MKN45 cells in vitro. The best anti-proliferative activity was observed for the C-

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Author

Jianqiang Deng; Xinyu Yang; Mingzhu Luan; Shuqi Liu; Juan Zhang; Sheng Jiang; Wenshui Wang; Guige Hou; Qingguo Meng; Hongbo Wang

Publisher

Bentham Science Publishers Ltd.

Published

2023

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)