Design and synthesis of new tetrandrine derivatives and their antitumor activities |
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Authors: | Xiao Wei Ting-Li Qu Yi-Fang Yang Jin-Fang Xu Xu-Wen Li |
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Affiliation: | 1. School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China;2. Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China;3. State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China |
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Abstract: | A series of tetrandrine derivatives were designed and synthesized using Suzuki coupling reaction. Eleven targeted compounds with over 50% inhibition against HL60 and A549 human cancer cell lines at 10 μM were further evaluated for the in vitro antitumor activities by MTT or SRB assay. The biological results revealed that some compounds exhibited potent antitumor activities. Thiophene derivative 6 and acetylphenyl derivative 5 were the most active ones against HL60 and A549 cell lines, with IC50 values less than 5 μM, which thus could be considered as useful candidate for further development of new antitumor agents. |
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Keywords: | Tetrandrine Suzuki coupling synthesis antitumor activity structure–activity relationship |
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