- Multicomponent Peptide Stapling as a Diversity-Driven Tool for the Development of Inhibitors of Protein–Protein Interactions
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Stapled peptides are chemical entities in-between biologics and small molecules, which have proven to be the solution to high affinity protein–protein interaction antagonism, while keeping control over pharmacological performance such as stability and mem
- Ali, Ameena M.,Atmaj, Jack,D?mling, Alexander,Groves, Matthew,Holak, Tad A.,Labuzek, Beata,Neochoritis, Constantinos G.,Plewka, Jacek,Ricardo, Manuel G.,Rivera, Daniel G.,Skalniak, Lukasz,Surmiak, Ewa,Zhang, Ran
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supporting information
p. 5235 - 5241
(2020/02/15)
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- Synthesis and antiproliferative activity of aromatic and aliphatic bis[aminomethylidene(bisphosphonic)] acids
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A series of aromatic and aliphatic bis[aminomethylidene(bisphosphonic)] acids was synthesized in the reaction of triethylphosphite with isonitriles followed by hydrolysis or dealkylation. The in vitro anti-proliferative effect of all synthesized tetraphosphonic acids against MCF-7 breast cancer cells, J774E macrophages and HL-60 promyelocytic leukemia cells was determined. Three aromatic derivatives (5a, 5f and 5j) showed a similar or higher anti-proliferative activity than zoledronic acid.
- Goldeman, Waldemar,Nasulewicz-Goldeman, Anna
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p. 3475 - 3479
(2014/07/22)
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- Rapid generation of macrocycles with natural-product-like side chains by multiple multicomponent macrocyclizations (MiBs)
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A small parallel library of peptoid macrocycles with natural-product- derived side chains of biological importance was produced by Ugi-type multiple multicomponent macrocyclizations including bifunctional building blocks (Ugi-MiBs). Diverse exocyclic elements of high relevance in natural recognition processes, i.e., all functional amino acid residues (e.g., Cys, Arg, His, Trp) and even sugar moieties, can be introduced in a one-pot process into different types of peptoid-containing macrocyclic skeletons. This is exemplified by the use of a diamine/diisocyanide combination of Ugi-MiBs and N-protected α-amino acids or carboxy-functionalized carbohydrates as source for the natural-product-like exocyclic elements. Employed as the acid components of the multiple Ugi reactions, they appear as N-amide substituents on the macrocyclic cores. The use of different diamines and diisocyanides allows an easy variation of the N- to C-directionality and therefore of the position of the exocyclic elements. The Royal Society of Chemistry.
- Rivera, Daniel G.,Vercillo, Otilie E.,Wessjohann, Ludger A.
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experimental part
p. 1787 - 1795
(2008/10/09)
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