2. Academic Validation
  3. Synthesis and structure-activity relationship studies of cytotoxic vinorelbine amide analogues

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

  • Bioorg Med Chem Lett. 2012 Dec 15;22(24):7547-50. doi: 10.1016/j.bmcl.2012.10.024.
Lingjun Hu 1,  Weibin Song,  Yuhui Meng,  Dean Guo,  Xuan Liu,  Lihong Hu
Affiliations

Affiliation

  • 1 College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, PR China.
PMID: 23107481 DOI: 10.1016/j.bmcl.2012.10.024
Abstract

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.

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