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  • Title: Combinatorial discovery of fluorescent pharmacophores by multicomponent reactions in droplet arrays.
    Author: Burchak ON, Mugherli L, Ostuni M, Lacapère JJ, Balakirev MY.
    Journal: J Am Chem Soc; 2011 Jul 06; 133(26):10058-61. PubMed ID: 21644551.
    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.
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