title: Combinatorial discovery of fluorescent pharmacophores by multicomponent reactions in droplet arrays.
abstract: Fluorescence imaging in clinical diagnostics and biomedical research relies to a great extent on the use of small organic fluorescent probes. Because of the difficulty of combining fluorescent and molecular-recognition properties, the development of such probes has been severely restricted to a number of well-known fluorescent scaffolds. Here we demonstrate that autofluorescing druglike molecules are a valuable source of bioimaging probes. Combinatorial synthesis and screening of chemical libraries in droplet microarrays allowed the identification of new types of fluorophores. Their concise and clean assembly by a multicomponent reaction presents a unique potential for the one-step synthesis of thousands of structurally diverse fluorescent molecules. Because they are based upon a druglike scaffold, these fluorophores retain their molecular recognition potential and can be used to design specific imaging probes.
authors.affiliation: Biomics Laboratory, Institut de Recherches en Technologies et Sciences pour le Vivant, CEA, 17 rue des Martyrs, 38054 Grenoble, France.
authors.forename: Olga N
authors.initials: ON
authors.lastname: Burchak
authors.forename: Laurent
authors.initials: L
authors.lastname: Mugherli
authors.forename: Mariano
authors.initials: M
authors.lastname: Ostuni
authors.forename: Jean Jacques
authors.initials: JJ
authors.lastname: Lacapère
authors.forename: Maxim Y
authors.initials: MY
authors.lastname: Balakirev
mesh_terms: D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D046228:Microarray Analysis / Q000379:methods*; D057054:Molecular Imaging; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D005456:Fluorescent Dyes; D054852:Small Molecule Libraries