Journal of Chemical Biology

, Volume 7, Issue 3, pp 85–91 | Cite as

Synthesis and investigation of new Hesperadin analogues antitumor effects on HeLa cells

  • Fereshteh Shamsipour
  • Saeeideh Hosseinzadeh
  • Seyed Shahriar Arab
  • Sedigheh Vafaei
  • Samira Farid
  • Mahmood Jeddi-Tehrani
  • Saeed Balalaie
Original Article

Abstract

Hesperadin is one of the indolinones that was designed against the ATP-binding site of Aurora kinase. This molecule inhibits Aurora B kinase by phosphorylation of histone H3. In this study, new derivatives of Hesperadin containing an amide group in their structures were synthesized through sequential Ugi/palladium-catalyzed approach and in vitro antitumor activity of new compounds were evaluated by cell proliferation assay. The results show that compounds 6f, 6i, 6l, and 6o were dose-dependently inhibited in different concentrations, and IC50 values were between 35 and 43 nM. It seems that lipophilic substitution on the indolinone core with the ability to form additional hydrogen bond might lead to increased stability of structure and activity of new Hesperadin analogues.

Keyword

Aurora kinase Hesperadin Antitumor effects Analogues 

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Copyright information

© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  • Fereshteh Shamsipour
    • 1
  • Saeeideh Hosseinzadeh
    • 2
  • Seyed Shahriar Arab
    • 3
  • Sedigheh Vafaei
    • 1
  • Samira Farid
    • 1
  • Mahmood Jeddi-Tehrani
    • 1
  • Saeed Balalaie
    • 2
  1. 1.Monoclonal Antibody Research CenterAvicenna Research Institute, ACECRTehranIran
  2. 2.Peptide Chemistry Research CenterK. N. Toosi University of TechnologyTehranIran
  3. 3.Department of Biophysics, School of Biological SciencesTarbiat Modares UniversityTehranIran

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