Diversity Oriented Synthesis 2016
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Molecular Diversity".
Deadline for manuscript submissions: closed (30 July 2016) | Viewed by 27276
Special Issue Editor
Interests: drug discovery; organic synthesis; medicinal chemistry; molecular imaging; diversity-oriented synthesis; peptidomimetics; chemoinformatics; enzyme inhibitors; angiogenesis; Alzheimer’s disease
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Since its introduction, Diversity-Oriented Synthesis (DOS) has become a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways, and to provide a larger array of the chemical space in drug discovery and chemical biology issues. This strategy combines the generation of a functionalized precursor with further synthetic elaborations, in order to generate the maximum diversity and complexity from simple starting material, thus achieving molecules that differ not only for the appendages, as in traditional combinatorial chemistry, but, also, in the stereochemistry and molecular skeleton. Several DOS approaches have been proposed thus far, as divergent pathways consisting of a complexity-generating reaction followed by cyclization steps and appendage diversity, or as synthetic schemes for generating different cyclic structures through the build/couple/pair approach.
The possibility of creating new highly-diverse and complex molecular platforms, and the achievement of hundreds to thousands to millions of compounds is producing significant advances in chemical biology and drug discovery. This is mainly due to the improvement of the quality of chemical libraries, which are more stereochemically rich and structurally complex. DOS molecular collections are being applied in high-throughput screening, phenotypic assays and chemical genetics studies, leading to the discovery of both new targets and new lead compounds.
To date, many research contributions regarding diversity-oriented synthesis, covering the organic and medicinal chemistry fields, have appeared in the literature. Nevertheless, this research area is quite vibrant and many research groups are active in this field.
We invite the submission of research articles or review papers on advances in diversity-oriented synthesis through the elaboration of novel molecular scaffolds, and innovative divergent synthetic pathways. Papers related to new technologies enabling library development or to chemoinformatic characterization of DOS collections are also welcome.
Prof. Dr. Andrea Trabocchi
Guest Editor
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Keywords
- Small molecules
- Building blocks
- Molecular diversity
- Combinatorial chemistry
- Drug discovery
- Chemical biology
- High-throughput screening
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