Synthesis, Anti-cancer Activity and Mechanism Study of 6-Mercapto-purine Derivatives

Author(s): Yu-qin Ma, Xing Yan, Rong Du, Xiao-guang Yang, Yu-xin Li, Ying Gao, Wen-liang Li

Journal Name: Letters in Drug Design & Discovery

Volume 13 , Issue 6 , 2016

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Graphical Abstract:


6-mercaptopurine (6-MP) is the first active metabolite inhibitor shown to suppress cancer cells. The aim of this study is to investigate the bioactivity of 6-MP derivatives and discover new anti-cancer agents. Four 6-mercaptopurine (6-MP) derivatives were synthesized and their anti-cancer activities were analyzed. All of the compounds showed anti-proliferative effects against HepG2 and A2780 cancer cells. Among the synthesized derivatives, 6-((naphthalen-2-ylmethyl)thio)-9H-purine (NMSP) which possessing a β-naphthalene, showed better anti-cancer activity than other compounds, with an IC50 value 6.09µg/mL. NMSP could induce S phase cell cycle arrest and apoptosis in HepG2 cells. Western blot analysis indicated that NMSP induced apoptosis is mitochondria-dependent. The novel 6-MP derivative discovered in this study is a promising drug candidate to be used as an anti-cancer agent.

Keywords: 6-mercaptopurine derivatives, synthesis, anti-cancer drugs, apoptosis, cell cycle, anti-proliferative.

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Article Details

Year: 2016
Page: [570 - 576]
Pages: 7
DOI: 10.2174/1570180812666150821003536
Price: $65

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