Tetrandrine derivatives IVa-IVd: Structural analysis and their inhibition rate against protein tyrosine kinase, and HL60 & A549 cancer cell lines

Chen, Chen ; Lu, Ye

Abstract

Four tetrandrine (TET) derivatives (IVa-IVd) have been synthesized by Suzuki reaction of boronic acid derivatives and 5-bromo-tetrandrine obtained by bromination using tetrandrine as the starting material. The structures are analyzed by 1H NMR, 13C NMR and ESI-MS. The inhibition activities of IVa-IVd against HL60 and A549 cancer cell lines have been investigated by CCK-8 assay. The compounds having significant (P <0.040) inhibition activities are secondarily screened by MTT assay. The inhibitory activities of IVa-IVd against protein tyrosine kinases (PTKs) are tested by ELISA. The results show that IVa, IVb and IVc exhibit significant inhibition activities against the two cancer cell lines. The IVb and IVc show highly significant (P <0.001) inhibition activities against fibroblast growth factor receptor 1 (FGFR1).


Keyword(s)

Anticancer; Bromination; CCK-8; FGFR1; PTKs; Suzuki reaction; Tetrandrine

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