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Paper | Regular issue | Vol 91, No. 2, 2015, pp.301-312
Published online, 22nd January, 2015
DOI: 10.3987/COM-14-13144
Design, Synthesis and Evaluation of Nitric Oxide-Releasing Derivatives of N-(n-Butyl)matrinic Acid And N-(n-Butyl)matrinol as Anti-Hepatocellular Carcinoma Agents

Ya-Xian Wu, Jun-Kai Huang, Lei-Lei Gao, Li-Qin He,* Peng Huang,* and Xiao-Shan Wang

*School of Pharmacy, Anhui University of Chinese Medicine, Yaohai District of Hefei City, Anhui Province, Mo Dian Xiang Anhui University of Chinese medicine shaoquan Lake Campus, 230012, China

Abstract

A series of novel furoxan-based derivatives of N-n-butyl matrinic acid (9a-m) and N-n-butyl matrinol (10a-m) were synthesized and their anti-human hepatocellular carcinoma (HCC) activities were evaluated. All derivatives displayed potential inhibition of HepG2 cell proliferation. Among these derivatives, compounds 9a-f, 9j and 10b, 10g-i (IC50: 0.69−4.66 μM) were superior to 5-FU (IC50: 5.82 μM). The further study showed that compounds 9a, 9c and 9f had higher antiproliferative activity on human hepatocellular carcinoma cells Bel-7402 (IC50: 2.55-3.26 μM) and SMMC-7721 (IC50: 5.26-5.79 μM).