Synthesis and structureaactivity relationship studies of cytotoxic vinorelbine amide analogues

A series of 3-demethoxycarbonyl-3-acylamide methyl vinorelbine derivatives (compounds 7aa7z) 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...

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Published inBioorganic & medicinal chemistry letters Vol. 22; no. 24; pp. 7547 - 7550
Main Authors Hu, Lingjun, Song, Weibin, Meng, Yuhui, Guo, Dean, Liu, Xuan, Hu, Lihong
Format Journal Article
LanguageEnglish
Published 15.12.2012
Subjects
amides
Cytotoxicity
Non-small cell lung carcinoma
Tumor cell lines
vinorelbine
Xenografts
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Summary:A series of 3-demethoxycarbonyl-3-acylamide methyl vinorelbine derivatives (compounds 7aa7z) 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.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2012.10.024