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Towards the optimal screening collection: a synthesis strategy.
| Publication Type | Journal Article |
| Authors | Nielsen, TE, and Schreiber SL |
| Abstract | The development of effective small-molecule probes and drugs entails at least three stages: 1) a discovery phase, often requiring the synthesis and screening of candidate compounds, 2) an optimization phase, requiring the synthesis and analysis of structural variants, 3) and a manufacturing phase, requiring the efficient, large-scale synthesis of the optimized probe or drug. Specialized project groups tend to undertake the individual activities without prior coordination; for example, contracted (outsourced) chemists may perform the first activity while in-house medicinal and process chemists perform the second and third development stages, respectively. The coordinated planning of these activities in advance of the first small-molecule screen tends not to be undertaken, and each project group can encounter a bottleneck that could, in principle, have been avoided with advance planning. Therefore, a challenge for synthetic chemistry is to develop a new kind of chemistry that yields a screening collection comprising small molecules that increase the probability of success in all three phases. Although this transformative chemistry remains elusive, progress is being made. Herein, we review a newly emerging strategy in diversity-oriented small-molecule synthesis that may have the potential to achieve these challenging goals. |
| Year of Publication | 2008 |
| Journal | Angewandte Chemie (International ed. in English) |
| Volume | 47 |
| Issue | 1 |
| Pages | 48-56 |
| Date Published (YYYY/MM/DD) | 2007/12/13 |
| ISSN Number | 1433-7851 |
| DOI | 10.1002/anie.200703073 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/18080276?dopt=Abstract |
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