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Citation: Mao Zewei, Wan Chunping, Zhang Mengdi, Zheng Xi, Rao Gaoxiong. Synthesis and Preliminary Antitumor Activity of Aza-Bergenin Derivatives[J]. Chemistry, ;2016, 79(4): 381-383. shu

Synthesis and Preliminary Antitumor Activity of Aza-Bergenin Derivatives

1.
1. School of Traditional Chinese Medicine, Yunnan University of Traditional Chinese Medicine, Kunming 650500;
2.
2. Central Laboratory, The NO. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021

Corresponding author: Rao Gaoxiong,
Received Date: 1 September 2015
Available Online: 14 November 2015
Fund Project:

Bergenin is attracting more and more attention due to its wide range of biological activities. In this work, eight aza-bergenin derivatives were synthesized by Mannich reaction and Mitsunobu reaction, and their structures were characterized by ¹H NMR, ¹³C NMR and HRMS. Their antitumor activities were studied in vitro against human tumor cell line A549 by the MTT assay. The results revealed that compound 3c and 3d are the most potential compounds against A549 (IC₅₀=3.74μmol/L and 5.05μmol/L, respectively), which showed better activity than bergenin and could be used as the lead compounds for further research.
- Bergenin,
- Derivatives,
- Synthesis,
- Anti-tumor activity
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