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. 2011 Jun 20;16(6):5130-41.
doi: 10.3390/molecules16065130.

Synthesis and cytotoxic evaluation of novel N-methyl-4-phenoxypicolinamide derivatives

Wei Li  1 , Xin Zhai, Lu Ding, Limin Sun, Xiaomei Chen, Ping Gong, Tiemin Sun
Affiliations

Synthesis and cytotoxic evaluation of novel N-methyl-4-phenoxypicolinamide derivatives

Wei Li et al. Molecules. .

Abstract

A series of N-methyl-4-phenoxypicolinamide derivatives were synthesized and evaluated in vitro for their cytotoxic activity against A549, H460 and HT29 cell lines. Pharmacological data indicated that some of the target compounds possessed marked antiproliferative activity, superior to that of the reference drug sorafenib. As the most promising compound, 8e exhibited potent cytotoxicity with the IC(50) value of 3.6, 1.7 and 3.0 μM against A549, H460 and HT-29 cell lines, respectively.

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Figures

Scheme 1
Scheme 1
Synthetic routes for 8a–8k and 10a–10e.
See this image and copyright information in PMC

References

    1. Liu L., Cao Y., Zhang X. Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. Clin. Cancer Res. 2006;66:11851–11858. - PubMed
    1. Wilhelm S.M., Advane L., Newell P. Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling. Mol. Cancer Ther. 2008;7:3129–3140. doi: 10.1158/1535-7163.MCT-08-0013. - DOI - PubMed
    1. Guida T., Anaganti S., Provitera L. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Cancer Res. 2007;13:3363–3369. doi: 10.1158/1078-0432.CCR-06-2667. - DOI - PubMed
    1. Potashman M.H., Bready J., Coxon A. Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors. J. Med. Chem. 2007;50:4351–4373. doi: 10.1021/jm070034i. - DOI - PubMed
    1. Ramurthy S., Subramanian S., Aikawa M. Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors. J. Med. Chem. 2008;51:7049–7052. doi: 10.1021/jm801050k. - DOI - PubMed

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