Biologically Orientated Synthesis in Drug Discovery

Several new paradigms, including biologically orientated synthesis and genomics, have been incorporated recently into the drug discovery process. The novel concept of biologically orientated synthesis, introduced in 2005 by Waldmann et al. [18, 19], is based on the following three essential aspects  

This concept is illustrated schematically in Fig. 1.3 [20]. This diagram summarizes the discovery of new modulators of both cell cycle progression and viral entry. The crux of the whole concept is the observation that Nature pairs nonpeptide small molecules with relevant protein receptors, and the number of binding-site topologies for small molecule ligands across aU protein families is limited. Phenotypic screening of the library of enantiopure a,p-unsaturated-8-lactones was exceptionally successful and has identified potent modulators of the two unrelated biological processes. In one case, the compounds are inhibitors of cell 

This approach is expected to improve and speed up the development of NDEs in many other therapeutic fields [21]. 

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