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.
Letters in Drug Design & Discovery
Title:Synthesis, Anti-cancer Activity and Mechanism Study of 6-Mercapto-purine Derivatives
Volume: 13 Issue: 6
Author(s): Yu-qin Ma, Xing Yan, Rong Du, Xiao-guang Yang, Yu-xin Li, Ying Gao and Wen-liang Li
Affiliation:
Keywords: 6-mercaptopurine derivatives, synthesis, anti-cancer drugs, apoptosis, cell cycle, anti-proliferative.
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.
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Cite this article as:
Ma Yu-qin, Yan Xing, Du Rong, Yang Xiao-guang, Li Yu-xin, Gao Ying and Li Wen-liang, Synthesis, Anti-cancer Activity and Mechanism Study of 6-Mercapto-purine Derivatives, Letters in Drug Design & Discovery 2016; 13 (6) . https://dx.doi.org/10.2174/1570180812666150821003536
DOI https://dx.doi.org/10.2174/1570180812666150821003536 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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