Synthesis and activity evaluation of benzoylurea derivatives as potential antiproliferative agents

…, KL Chen, GF Wang, P Yang, LZ Wu, XB Zhang…

文献索引：Song, Dan-Qing; Wang, Yue-Ming; Du, Na-Na; He, Wei-Ying; Chen, Ke-Liang; Wang, Gui-Fang; Yang, Peng; Wu, Lian-Zong; Zhang, Xue-Bo; Jiang, Jian-Dong Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 755 - 758

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被引用次数: 11

摘要

3-Haloacylamino benzoylureas (3-HBUs) consist of a new family of tubulin ligands that kill cancer cells through mitotic arrest. In exploring the structure–activity relationship (SAR), 17 analogues defined through variations of formylurea at the 1-position of the aromatic ring were synthesized. SAR analysis revealed that (i) the p–π conjugation between the aromatic ring and formylurea was essential;(ii) suitable aryl substitutions at the N′-end increased ...