Russian Journal of General Chemistry

, Volume 86, Issue 12, pp 2891–2899 | Cite as

Biological evaluation of 4-aryl-1,4-dihydropyridines as VEGFR-2 kinase inhibitors

  • W. Sun
  • Z. Ma
  • H. YanEmail author


Vascular endothelial growth factor-2 receptor (VEGFR-2) kinase is a promising target for the development of novel anticancer drugs. Molecular docking modeling was performed on a series of 4-aryl-1,4-dihydropyridines derivatives to evaluate the structural basis for VEGFR-2 inhibitory activity. Some 4-aryl-1,4-dihydropyridines were synthesized in the reaction of aromatic aldehydes and ethyl propiolate with anilines in acetic acid. The biological activities were evaluated against the cells A549, A431 and Hep-G2. The results indicated that 4-aryl-1,4-dihydropyridines could be the promising potential VEGFR-2 inhibitors.


VEGFR-2 inhibitors 4-aryl-1,4-dihydropyridines molecular docking biological activity 


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  1. 1.
    Vajkoczy, P., Farhadi, M., Gaumann, A., Heidenreich, R., Erber, R., Wunder, A., Tonn, J.C.M.D., Menger, G., J. Clin. Invest., 2002, vol. 109, p. 777.CrossRefGoogle Scholar
  2. 2.
    McMahon, G., Oncologist, 2000, vol. 5, p. 3.CrossRefGoogle Scholar
  3. 3.
    Strawn, L.M., McMahon, G., App, H., Schreck, R., Kuchler, W.R., Longhi, M.P., Hui, T.H., Tang, C., Levitzki, A., and Gazit, A., Cancer Res., 1996, vol. 56, p. 3540.PubMedGoogle Scholar
  4. 4.
    Eckstein, N., Röper, L., Haas, B., Potthast, H., Hermes, U., Unkrig, C., Naumann-Winter, F., and Enzmann, H., J. Exp. Clin. Cancer Res., 2014, vol. 33, p. 15.CrossRefGoogle Scholar
  5. 5.
    Eldehna, W.M., Fares, M., Ibrahim, H.S., Aly, M.H., Zada, S., Ali, M.M., Abou-Seri, S.M., Abdel-Aziz, H.A., and El Ella, D.A.A., Eur. J. Med. Chem., 2015, vol. 100, p. 89.CrossRefGoogle Scholar
  6. 6.
    Zhong, H., Wang, D., Wang, N., Rios, Y., Huang, H., Li, S., Wu, X., and Lin, S., Cell Res., 2011, vol. 21, p. 1080.CrossRefGoogle Scholar
  7. 7.
    Borzilleri, R.M. and Cai, Z.W., WO Patent 2009094417, 2009.Google Scholar
  8. 8.
    Chen, Y., Huang, Y., Reiberger, T., Duyverman, A.M., Huang, P., Samuel, R., Hiddingh, L., Roberge, S., Koppel, C., Lauwers, G.Y., Zhu, A.X., Jain, R.K., and Duda, D.G., Hepatology, 2014, vol. 59, p. 1435.CrossRefGoogle Scholar
  9. 9.
    Jonas, M., Goldbourt, U., Boyko, V., Mandelzweig, L., Behar, S., and Reicher-Reiss, H., Cardiovasc. Drugs Ther., 1998, vol. 12, p. 177.CrossRefGoogle Scholar
  10. 10.
    Yang, Z., Niu, H.Y., Lan, Y.H., and Fu, B.W., Labor. Med. Clin., 2014, vol. 9, p. 024.Google Scholar
  11. 11.
    Tsai, J.Y., Chou, C.T., Liu, S.I., Liang, W.Z., Kuo, C.C., Liao, W.C., Lin, K.L., Hsu, S.S., Lu, Y.C., and Huang, J.K., J. Recept. Sign. Transd., 2012, vol. 32, p. 271.CrossRefGoogle Scholar
  12. 12.
    Kuo, G.H., Prouty, C., Wang, A., Emanuel, S., DeAngelis, A., Zhang, Y., Song, F., Beall, L., Connolly, P.J., and Karnachi, P., J. Med. Chem., 2005, vol. 48, p. 4892.CrossRefGoogle Scholar
  13. 13.
    Munchhof, M.J., Beebe, J.S., Casavant, J.M., Cooper, B.A., Doty, J.L., Higdon, R.C., Hillerman, S.M., Soderstrom, C.I., Knauth, E.A., and Marx, M.A., Bioorg. Med. Chem. Lett., 2004, vol. 14, p. 21.CrossRefGoogle Scholar
  14. 14.
    Oguro, Y., Cary, D.R., Miyamoto, N., Tawada, M., Iwata, H., Miki, H., Hori, A., and Imamura, S., Bioorg. Med. Chem., 2013, vol. 21, p. 4714.CrossRefGoogle Scholar
  15. 15.
    Morris, G.M., Huey, R., and Olson, A.J., Curr. Protocols in Bioinform., 2008, vol. 8, p. 14.Google Scholar
  16. 16.
    Chennat, T. and Eisner, U., J. Chem. Soc., 1975, p. 926.Google Scholar
  17. 17.
    Sueki, S., Takei, R., Zaitsu, Y., Abe, J., Fukuda, A., Seto, K., Furukawa, Y., and Shimizu, I., Eur. J. Org. Chem., 2014, vol. 2014, p. 5281.CrossRefGoogle Scholar
  18. 18.
    Darzynkiewicz, Z. and Bedner, E., Methods in Enzymol., 2000, vol. 322, p. 18.CrossRefGoogle Scholar
  19. 19.
    Fiebig, H., Maier, A., and Burger, A., Eur. J. Cancer, 2004, vol. 40, p. 802.CrossRefGoogle Scholar

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© Pleiades Publishing, Ltd. 2016

Authors and Affiliations

  1. 1.College of Life Science and BioengineeringBeijing University of TechnologyBeijingChina

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