Design and Synthesis of Fsp3-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening | Zendy

Silvia Stotani | Zendy; Christoph Lorenz | Zendy; Mathias Winkler | Zendy; Federico Medda | Zendy; Edwige Picazo | Zendy; Raquel Ortega Martinez | Zendy; Anna Karawajczyk | Zendy; Jorge SánchezQuesada | Zendy; Fabrizio Giordanetto | Zendy

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Design and Synthesis of Fsp³-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening

Author(s) -

Silvia Stotani,

Christoph Lorenz,

Mathias Winkler,

Federico Medda,

Edwige Picazo,

Raquel Ortega Martinez,

Anna Karawajczyk,

Jorge SánchezQuesada,

Fabrizio Giordanetto

Publication year - 2016

Publication title -

acs combinatorial science

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.928

H-Index - 81

eISSN - 2156-8952

pISSN - 2156-8944

DOI - 10.1021/acscombsci.6b00005

Subject(s) - chemistry , chemical space , combinatorial chemistry , drug discovery , reagent , chemical synthesis , nanotechnology , organic chemistry , biochemistry , materials science , in vitro

The exploration of innovative chemical space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biologically relevant metabolites and show attractive features, such as molecular compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available commercial reagents and robust chemical transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented.

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