1. Synthesis, Characterization and Activity Evaluation of Matrinic Acid Derivatives as Potential Antiproliferative Agents
- Author
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Dong-En Wang, Fan Chao, Jinyi Wang, Jian-Jun Liu, Qin Tu, and Rui Liu
- Subjects
antiproliferative activity ,synthesis ,Stereochemistry ,Electrospray ionization ,Pharmaceutical Science ,Acids, Carbocyclic ,Antineoplastic Agents ,Mass spectrometry ,Article ,Analytical Chemistry ,lcsh:QD241-441 ,HeLa ,Alkaloids ,lcsh:Organic chemistry ,matrinic acid derivative ,Drug Discovery ,Humans ,Physical and Theoretical Chemistry ,Matrines ,Cell Proliferation ,A549 cell ,biology ,Chemistry ,Organic Chemistry ,Hep G2 Cells ,biology.organism_classification ,In vitro ,Chemistry (miscellaneous) ,Hepg2 cells ,Antiproliferative Agents ,Molecular Medicine ,Drug Screening Assays, Antitumor ,Quinolizines ,Nuclear chemistry ,HeLa Cells - Abstract
A series of new matrinic acid derivatives 5a–e was synthesized. The chemical structures of the synthesized compounds were confirmed by 1H-NMR, 13C-NMR, and electrospray ionization mass spectroscopy. The anti-tumor activities were also investigated in vitro by evaluating the effect of synthesized compounds on the proliferation of A375, A549, HeLa, and HepG2 cells. Compound 5e was found to be the most potent against A375 and HeLa cells, with IC50 values of 37 and 75.5 μg/mL, respectively. Compounds 5b, 5c, 5g, and 5h also exhibited antiproliferative activities against A549 cells, with IC50 values within the 36.2–47 μg/mL range. For HepG2 cells, 5e and 5i, with IC50 values of 78.9 and 61 μg/mL, respectively, showed higher antiproliferative activity than taxol.
- Published
- 2013