Synthesis and structure-activity relationship studies of cytotoxic vinorelbine amide analogues

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• 作者：Lingjun Hu^b ; ^&dagger ; ; Weibin Song^a ; ^&dagger ; ; Yuhui Meng^a ; Dean Guo^a ; Xuan Liu^a ; ^{xuanliu@mail.shcnc.ac.cn} ; Lihong Hu^a ; ^b ; ^{simmhulh@mail.shcnc.ac.cn}
• 关键词：Vinorelbine ; C-22 amide analogues ; Tubulin inhibitor ; Structure&ndash ; activity relationship (SAR) ; Cytotoxicity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 December, 2012
• 年：2012
• 卷：22
• 期：24
• 页码：7547-7550
• 全文大小：2209 K

文摘

A series of 3-demethoxycarbonyl-3-acylamide methyl vinorelbine derivatives (compounds 7a-7z) were designed, synthesized, and evaluated for their inhibition activities against human non-small cell lung cancer cell line (A549). Most of the amide derivatives exhibited potent cytotoxicity, with the size of the introduced substituents being the foremost factor in determining the resultant cytotoxic activity. Test results in vivo against nude mice bearing A549 xenografts indicated that 7y showed comparable activities compared to the parent NVB.