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

Autor:	Alexander G. Tonevitsky, Alexander G. Majouga, Maksim E. Kukushkin, Mark S. Veselov, Yan A. Ivanenkov, Alexey E. Machulkin, Elena K. Beloglazkina, Nina V. Chufarova, Elizaveta S. Chernyaginab, Sergei V. Vasilevski, Anton S. Vanzcool, Nikolay V. Zyk, Olga A. Dontsova, Alexander L. Rusanov, Dmitry A. Skvortsov, A. A. Khutornenko
Rok vydání:	2015
Předmět:	Models Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Molecular Dynamics Simulation Biochemistry Small Molecule Libraries Structure-Activity Relationship Neoplasms Drug Discovery Tumor Cells Cultured Humans Mdm2 p53 Molecular Biology Cell Proliferation Biological evaluation Molecular Structure Chemistry Organic Chemistry Diastereomer Regioselectivity Proto-Oncogene Proteins c-mdm2 Combinatorial chemistry Small molecule Design synthesis Drug Design Molecular Medicine Tumor Suppressor Protein p53
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 25:404-409
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2014.09.070
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d71a35c33dc5f8bd5b763db333a04ed https://doi.org/10.1016/j.bmcl.2014.09.070 Zobrazit plný text záznamu Full Text from ScienceDirect