A New Review Paper by Enamine’s Scientists: "The Symbiotic Relationship Between Drug Discovery and Organic Chemistry”


The review mentioned in the title was published in Chemistry – A European journal and emerged from a collaboration of scientists from Enamine Ltd. (including myself) and Duncan Judd from Awridian Ltd. Despite some “symbiotic” hype in the title (as it was pointed out by one of the reviewers), the paper provides a comprehensive overview of concepts which appeared at the edge of these disciplines recently. Initially, we have aimed at tutorial review that might help synthetic chemists to become familiar with state-of-the-art in the field. Thus, genesis of concepts like “…-oriented” syntheses (DOS, LOS, BIOS, FOS, DTS), as well as related “abbreviated” strategies (BBs, FBDD, DEL, REAL) has been discussed, together with recent advances focusing mainly on chemical aspects.


However, the paper exceeded the initial “tutorial” goal, and in my opinion, it might be of interest not only to beginners in the field, but also to highly qualified specialists in medicinal chemistry and related sciences. Although we attempted to be as neutral as possible, one might feel that we advocated for the compound selection models taking into account physico-chemical properties of the compounds, and hence concepts like lead-oriented-synthesis (LOS). Despite recent criticism and numerous successful exceptions, we believe that if used properly, such strategies might be step at the right direction for early drug discovery. In particular, LOS-like concepts seem to be dominating for building blocks, and majority of the Enamine’s building block collection have been designed by the corresponding criteria such as “the smaller, the better”.


The title picture (which was also used as a frontispiece for the paper) shows one of the most beautiful examples of symbiosis found in Nature – a hummingbird pollinating an ornithophilous flower. These two families co-evolved together, changing their features (i.e. the bill shape of the bird, as well as color spectrum and nectar composition of the plant) to get maximum benefit from their interaction. This is a good illustration of the main concept of the paper: similar symbiotic relationship between synthetic organic chemistry and early drug discovery exists.


For further information, read the full paper at Wiley’s website.

A New Paper by Enamine’s Scientists: "Synthesis an...
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