2,30-Bis(10H-indole) heterocycles: New p53/MDM2/MDMX antagonists

Autor:	Constantinos G, Neochoritis, Kan, Wang, Natalia, Estrada-Ortiz, Eberhardt, Herdtweck, Katarzyna, Kubica, Aleksandra, Twarda, Krzysztof M, Zak, Tad A, Holak, Alexander, Dömling
Rok vydání:	2015
Předmět:	Molecular Docking Simulation Binding Sites Indoles Heterocyclic Compounds Fluorescence Polarization Protein Interaction Domains and Motifs Proto-Oncogene Proteins c-mdm2 Tumor Suppressor Protein p53 Article Protein Structure Tertiary
Zdroj:	Bioorganicmedicinal chemistry letters. 25(24)
ISSN:	1464-3405
Popis:	The protein-protein interaction of p53 and MDM2/X is a promising non genotoxic anticancer target. A rapid and efficient methodology was developed to synthesize the 2,3'-bis(1'H-indole) heterocyclic scaffold 2 as ester, acid and amide derivatives. Their binding affinity with MDM2 was evaluated using both fluorescence polarization (FP) assay and HSQC experiments, indicating good inhibition and a perfect starting point for further optimizations.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::7f9819fc93c8a2d076018e749dc8ac9a https://pubmed.ncbi.nlm.nih.gov/26584879 Zobrazit plný text záznamu Full Text from ScienceDirect