title: Discovery of protein-protein binding disruptors using multi-component condensations small molecules.
abstract: A series of small molecule compounds interfering with the binding process of VEGF and NRP1 has been identified and further optimized. Full synthetic details as well as SAR are reported which demonstrate that expeditious MCC-based syntheses may lead to valuable molecules addressing challenging targets such as protein-protein interactions. Preliminary functional assay data confirm that these compounds may be further developed toward drug candidates.
authors.affiliation: Pierre Fabre Urologie, 11 Av. Albert Einstein, 69100 Villeurbanne, France.
authors.forename: Karim
authors.initials: K
authors.lastname: Bedjeguelal
authors.forename: Hugues
authors.initials: H
authors.lastname: Bienaymé
authors.forename: Antoine
authors.initials: A
authors.lastname: Dumoulin
authors.forename: Stéphane
authors.initials: S
authors.lastname: Poigny
authors.forename: Philippe
authors.initials: P
authors.lastname: Schmitt
authors.forename: Eric
authors.initials: E
authors.lastname: Tam
mesh_terms: D002460:Cell Line; D039942:Neuropilin-1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011485:Protein Binding; D013329:Structure-Activity Relationship; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D042461:Vascular Endothelial Growth Factor A; D039942:Neuropilin-1