Synthesis, Characterization and Activity Evaluation of Matrinic Acid Derivatives as Potential Antiproliferative Agents

Author： Chao Fan   Wang Dong-En   Liu Rui   Tu Qin   Liu Jian-Jun   Wang Jinyi  

Publisher： MDPI

E-ISSN： 1420-3049|18|5|5420-5433

ISSN： 1420-3049

Source： Molecules, Vol.18, Iss.5, 2013-05, pp. : 5420-5433

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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.

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