Design, synthesis and biological evaluation of novel potent MDM2/p53 small-molecule inhibitors. Issue 2 (15th January 2015)

• Record Type: Journal Article
• Authors: Ivanenkov, Yan A.; Vasilevski, Sergei V.; Beloglazkina, Elena K.; Kukushkin, Maksim E.; Machulkin, Alexey E.; Veselov, Mark S.; Chufarova, Nina V.; Chernyaginab, Elizaveta S.; Vanzcool, Anton S.; Zyk, Nikolay V.; Skvortsov, Dmitry A.; Khutornenko, Anastasia A.; Rusanov, Alexander L.; Tonevitsky, Alexander G.; Dontsova, Olga A.; Majouga, Alexander G.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 2(2015)
• Page Start: 404
• Page End: 409
• Publication Date: 2015-01-15
• Subjects: MDM2/p53 -- PPI inhibitors -- Dispiro-indolinones -- 3D molecular docking -- Cell-based assay; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2014.09.070
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Regioselective synthesis, biological evaluation and 3D-molecular modeling for a series of novel diastereomeric 2-thioxo-5 H -dispiro[imidazolidine-4, 3-pyrrolidine-2, 3-indole]-2, 5(1 H )-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.