13 research outputs found
Design of indole- and MCR-based macrocycles as p53-MDM2 antagonists
Get PDFMacrocycles were designed to antagonize the protein-protein interaction p53-MDM2 based on the three-finger pharmacophore F19W23L25. The synthesis was accomplished by a rapid, one-pot synthesis of indole-based macrocycles based on Ugi macrocyclization. The reaction of 12 different α,ω-amino acids and different indole-3-carboxaldehyde derivatives afforded a unique library of macrocycles otherwise difficult to access. Screening of the library for p53-MDM2 inhibition by fluorescence polarization and 1H,15N HSQC NMR measurements confirm MDM2 binding
Structure and Reactivity of Glycosyl Isocyanides
Get PDF3D structural information was obtained from mono-, di- and trisaccharide formamide and isocyanide derivatives by analysis of their X-ray crystal structure and NMR spectroscopy. The isocyanide anomeric effect was observed. Data mining of the Cambridge Structural Database (CSD) was performed and statistically confirmed our findings. Application of the glycoside isocyanides in the synthesis of novel glycoconjugates as drug-like scaffolds by MCR chemistry underscores the usefulness of the novel building blocks
CCDC 1869941: Experimental Crystal Structure Determination
No full textRelated Article: Constantinos Neochoritis, Ehsan Ghonchepour, Maryam Kazemi Miraki, Tryfon Zarganes-Tzitzikas, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Doemling|2018|Eur.J.Org.Chem.|2018|50|doi:10.1002/ejoc.20180158
CCDC 1870510: Experimental Crystal Structure Determination
No full textRelated Article: Constantinos Neochoritis, Ehsan Ghonchepour, Maryam Kazemi Miraki, Tryfon Zarganes-Tzitzikas, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Doemling|2018|Eur.J.Org.Chem.|2018|50|doi:10.1002/ejoc.20180158
CCDC 1869944: Experimental Crystal Structure Determination
No full textRelated Article: Constantinos Neochoritis, Ehsan Ghonchepour, Maryam Kazemi Miraki, Tryfon Zarganes-Tzitzikas, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Doemling|2018|Eur.J.Org.Chem.|2018|50|doi:10.1002/ejoc.20180158
CCDC 1869945: Experimental Crystal Structure Determination
No full textRelated Article: Constantinos Neochoritis, Ehsan Ghonchepour, Maryam Kazemi Miraki, Tryfon Zarganes-Tzitzikas, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Doemling|2018|Eur.J.Org.Chem.|2018|50|doi:10.1002/ejoc.20180158
CCDC 1869946: Experimental Crystal Structure Determination
No full textRelated Article: Constantinos Neochoritis, Ehsan Ghonchepour, Maryam Kazemi Miraki, Tryfon Zarganes-Tzitzikas, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Doemling|2018|Eur.J.Org.Chem.|2018|50|doi:10.1002/ejoc.20180158
CCDC 1870511: Experimental Crystal Structure Determination
No full textRelated Article: Constantinos Neochoritis, Ehsan Ghonchepour, Maryam Kazemi Miraki, Tryfon Zarganes-Tzitzikas, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Doemling|2018|Eur.J.Org.Chem.|2018|50|doi:10.1002/ejoc.20180158
CCDC 1870509: Experimental Crystal Structure Determination
No full textRelated Article: Constantinos Neochoritis, Ehsan Ghonchepour, Maryam Kazemi Miraki, Tryfon Zarganes-Tzitzikas, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Doemling|2018|Eur.J.Org.Chem.|2018|50|doi:10.1002/ejoc.20180158
