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1, 1-Diarylalkenes as anticancer agents: Dual inhibitors of tubulin polymerization and phosphodiesterase 4

AL Ruchelman, HW Man, R Chen, W Liu, L Lu…

文献索引：Ruchelman, Alexander L.; Man, Hon-Wah; Chen, Roger; Liu, Wei; Lu, Ling; Cedzik, Dorota; Zhang, Ling; Leisten, Jim; Collette, Alice; Narla, Rama Krishna; Raymon, Heather K.; Muller, George W. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 21 p. 6356 - 6374

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被引用次数: 8

摘要

A series of 1, 1-diarylalkene derivatives were prepared to optimize the properties of CC- 5079 (1), a dual inhibitor of tubulin polymerization and phosphodiesterase 4 (PDE4). By using the 3-ethoxy-4-methoxyphenyl PDE4 pharmacophore as one of the aromatic rings, a significant improvement in PDE4 inhibition was achieved. Compound 28 was identified as a dual inhibitor with potent PDE4 (IC50= 54nM) and antitubulin activity (HCT-116 IC50= ...

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