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

• Main Authors: Jian-Jun Liu, Qin Tu, Rui Liu, Dong-En Wang, Fan Chao, Jinyi Wang
• Format: Article
• Language: English
• Published: MDPI AG 2013-05-01
• Series: Molecules
• Subjects: matrinic acid derivative; synthesis; antiproliferative activity
• Online Access: http://www.mdpi.com/1420-3049/18/5/5420

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.