About this Research Topic
Since Stuart Schreiber published his seminal work on the Diversity Oriented approach in the journal Science in 2000, it has received more than 1600 citations, and Schreiber’s vision has shaped many scientists’ work all over the world.
Diversity Oriented Synthesis (DOS) of small organic molecules has emerged as a powerful tool to explore the interface between chemistry and biology. Diversity oriented methodologies aim to generate molecular complexity, providing new molecular entities inspired by natural products that may or may not contain their original scaffolds. This can lead—and indeed has led—to the discovery of bioactive molecules for new and challenging targets, through an interdisciplinary approach including computational methods.
In the new millennium, everything becomes quickly obsolete. It is therefore reasonable to question whether the Diversity Oriented Synthesis approach is still valid or is experiencing a contraction, after its explosion at the beginning of this century. The answer to this question is clear: since 2011, the number of publications with DOS as the main topic has increased each year, according to Web of Science. On average, every single day a paper dealing with Diversity Oriented Synthesis is published in a peer-reviewed journal.
However, there is a question that is not so easy to answer: has the concept of Diversity Oriented Synthesis remained unchanged over these two decades, or do we observe improvements or deviations from the original guidelines drawn by the pioneers? Is there a new (second) generation of Diversity Oriented chemists that is exploring new possibilities, expanding original concepts, implementing computational approaches, and taking DOS in new directions or on new paths?
The aim of this Research Topic is to collect contributions on the state-of-the-art and progress of Diversity Oriented Synthesis, and to foresee its shape in the next decade. We therefore welcome high-quality original research and review papers addressing this topic.
Keywords: Diversity Oriented Synthesis, Combinatorial Chemistry, Molecular Complexity, Natural Products, Forward Synthetic Analysis
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