Synthesis and biological evaluation of heteroaryl styryl sulfone derivatives as anticancer agents

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• 作者：Yi Long ; Mingfeng Yu ; Peng Li ; Saiful Islam ; Aik Wye Goh ; Malika Kumarasiri ; Shudong Wang ; ^{shudong.wang@unisa.edu.au" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Kinase inhibitor ; Polo-like kinase 1 ; Ras-driven signaling pathways ; Non-ATP competitive inhibition ; Anti-cancer agents
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 December 2016
• 年：2016
• 卷：26
• 期：23
• 页码：5674-5678
• 全文大小：1138 K

文摘

Herein we disclose a series of novel heteroaryl styryl sulfone derivatives as potential anticancer agents. Structure-activity relationships of these newly synthesised compounds were explored with respect to the significance of the position and number of nitrogen atom of the heteroaryl ring for anti-proliferative activity in human cancer cell lines. A lead compound 14f was tested against a panel of cancerous and untransformed cell lines, and found to be highly potent against cancer cells with minimal toxicity in the untransformed cells. Further mechanistic studies uncovered that 14f caused cell-cycle arrest at the G2/M phase and induced apoptosis by targeting CDC25C and Mcl-1 proteins in A2780 ovarian cells.