BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer. Structural analogy of early methyl-triazolo BET inhibitors has prompted a need for structurally dissimilar ligands as probes of bromodomain function. Using fluorous-tagged multicomponent reactions, we developed a focused chemical library of bromodomain inhibito...

Åkerbladh, L. 2017. Palladium(0)-Catalysed Carbonylative Multicomponent Reactions. Synthesis of Heterocycles and the Application of Quinolinyl Pyrimidines as Enzyme Inhibitors. Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Pharmacy 237. 86 pp. Uppsala: Acta Universitatis Upsaliensis. ISBN 978-91-513-0083-2. Palladium-catalysed carbonylative multicomponent reaction...

a mild and efficient one-pot three-component and environmentally benign approach for the synthesis of a wide range of hydantoin annulated derivatives has been described. a multi-component reaction between a carbonyl compounds (ketone or aldehyde), potassium cyanide and ammonium carbonate (as cyanating agent and amine source, respectively leads to the formation of hydantoins. the proposed optimi...

in this study, the synthesis of 4 h -chromenes of biological activity via a multicomponent reaction of dimedone, aromatic aldehydes and malononitrile catalyzed by glutamic acid as a catalyst was investigated. the structural features of the synthesized compounds were characterized by melting point, ir and 1 h nmr analysis. the catalyst being reported here is cheap, safe to handle and the whole p...

Multicomponent reactions are one of the most interesting concepts in modern synthetic chemistry and, as shown in this critical review, they provide an attractive entry into pyrrole derivatives, which are very important heterocycles from many points of view including medicinal and pharmaceutical chemistry and materials science (97 references).

The development of new practical and green methods for the synthesis of small heterocycles is an attractive area of research due to the well-known potential of heterocyclic small molecule scaffolds in the drug discovery process. Herein we report a one-pot, three-component sequential procedure for the synthesis of diversely 1,3,5- and 1,3,5,5-substituted hydantoins, in high yields and very mild ...