Synthesis of Novel Tetrandrine Derivatives and Their Biological Activities
WEI Xiao1, YANG Yi-fang2, ZHAO Zheng-bao1
1.School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China； 2. Shanghai Institute of Pharmaceutical Industry, Shanghai, 200040, China
Abstract：Six novel tetrandrine derivatives(4a~4f) were synthesized by Suzuki coupling reaction of boronic acid derivatives and 5-bromotetrandrine， which was obtained by bromination, using tetrandrine as the starting material. The structures were characterized by 1H NMR, 13C NMR and ESI-MS. The inhibition activities of 4a~4f against A549 and HL60 cancer cell lines were investigated by CCK-8 assay. The compounds which had better inhibition activities were secondary screened by MTT assay. The inhibitory activities of 4a~4f against PTKs were tested by ELISA. The results showed that 4b, 4c and 4e exhibited well inhibition activities against the two cancer cell lines. 4b and 4c showed better inhibition activities against FGFR1.
2016, Vol. 24 
