Three Efficient Methods for Preparation of Coelenterazine Analogues.

作者: Anton Shakhmin , Mary P. Hall , Joel R. Walker , Thomas Machleidt , Brock F. Binkowski

DOI: 10.1002/CHEM.201601111

关键词: Structural diversityBioluminescent AssaysChemistryBioluminescenceReaction conditionsCombinatorial chemistryBioorganic chemistryCoelenterazine

摘要: The growing popularity of bioluminescent assays has highlighted the need for coelenterazine analogues possessing properties tuned specific applications. However, structural diversity known been limited by current syntheses. Known routes preparation employ harsh reaction conditions that limit access to many substituents and functional groups. Novel synthetic reported here establish simple robust methods synthesis investigation structurally diverse marine luciferase substrates. Specifically, these new allow containing various heterocyclic motifs substituted aromatic groups with electronic at R(2) position. Interesting described herein were characterized their physicochemical properties, half-life, light output, polarity cytotoxicity. Some represent leads can be utilized in development improved systems.

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