Design of indole- and MCR-based macrocycles as p53-MDM2 antagonists
Copyright policy )Design of indole- and MCR-based macrocycles as p53-MDM2 antagonists
Macrocycles 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.
- University of Groningen Netherlands
- Jagiellonian University Poland
- FACULTY OF CHEMISTRY Poland
- Tarbiat Modares University Iran (Islamic Republic of)
- University of Gronigen Netherlands
p53-MDM2, Science, Q, CONCISE SYNTHESIS, Organic chemistry, multicomponent, ARTIFICIAL MACROCYCLES, Full Research Paper, Ugi reaction, macrocycles, QD241-441, MDM2, indole, MULTICOMPONENT REACTIONS, DISCOVERY, BIND, DRUGS, INHIBITORS, 1H,15N HSQC NMR
p53-MDM2, Science, Q, CONCISE SYNTHESIS, Organic chemistry, multicomponent, ARTIFICIAL MACROCYCLES, Full Research Paper, Ugi reaction, macrocycles, QD241-441, MDM2, indole, MULTICOMPONENT REACTIONS, DISCOVERY, BIND, DRUGS, INHIBITORS, 1H,15N HSQC NMR
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