Design, synthesis and biological evaluation of novel potent MDM2/p53 small-molecule inhibitors

Yan A. Ivanenkov, Sergei V. Vasilevski, Elena K. Beloglazkina, Maksim E. Kukushkin, Alexey E. Machulkin, Mark S. Veselov, Nina V. Chufarova, Elizaveta S. Chernyaginab, Anton S. Vanzcool, Nikolay V. Zyk, Dmitry A. Skvortsov, Anastasia A. Khutornenko, Alexander L. Rusanov, Alexander G. Tonevitsky, Olga A. Dontsova, Alexander G. Majouga

Research output: Contribution to journalArticlepeer-review

44 Citations (Scopus)

Abstract

Regioselective synthesis, biological evaluation and 3D-molecular modeling for a series of novel diastereomeric 2-thioxo-5H-dispiro[imidazolidine-4,3-pyrrolidine-2,3-indole]-2,5(1H)-diones are described. The studied compounds have been tentatively identified as potent small molecule MDM2/p53 PPI inhibitors and can therefore be reasonably regarded as promising anticancer therapeutics.

Original languageEnglish
Pages (from-to)404-409
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number2
DOIs
Publication statusPublished - 15 Jan 2015
Externally publishedYes

Keywords

  • 3D molecular docking
  • Cell-based assay
  • Dispiro-indolinones
  • MDM2/p53
  • PPI inhibitors

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