Title |
A unified lead-oriented synthesis of over fifty molecular scaffolds
|
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Published in |
Organic and Biomolecular Chemistry, January 2015
|
DOI | 10.1039/c4ob02287d |
Pubmed ID | |
Authors |
Richard G. Doveston, Paolo Tosatti, Mark Dow, Daniel J. Foley, Ho Yin Li, Amanda J. Campbell, David House, Ian Churcher, Stephen P. Marsden, Adam Nelson |
Abstract |
Controlling the properties of lead molecules is critical in drug discovery, but sourcing large numbers of lead-like compounds for screening collections is a major challenge. A unified synthetic approach is described that enabled the synthesis of 52 diverse lead-like molecular scaffolds from a minimal set of 13 precursors. The divergent approach exploited a suite of robust, functional group-tolerant transformations. Crucially, after derivatisation, these scaffolds would target significant lead-like chemical space, and complement commercially-available compounds. |
X Demographics
Geographical breakdown
Country | Count | As % |
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United Kingdom | 5 | 50% |
New Zealand | 1 | 10% |
United States | 1 | 10% |
Unknown | 3 | 30% |
Demographic breakdown
Type | Count | As % |
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Scientists | 6 | 60% |
Members of the public | 4 | 40% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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United Kingdom | 1 | 1% |
France | 1 | 1% |
Unknown | 76 | 97% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 21 | 27% |
Researcher | 14 | 18% |
Student > Master | 12 | 15% |
Student > Bachelor | 11 | 14% |
Other | 4 | 5% |
Other | 7 | 9% |
Unknown | 9 | 12% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 58 | 74% |
Biochemistry, Genetics and Molecular Biology | 2 | 3% |
Agricultural and Biological Sciences | 2 | 3% |
Computer Science | 2 | 3% |
Pharmacology, Toxicology and Pharmaceutical Science | 1 | 1% |
Other | 1 | 1% |
Unknown | 12 | 15% |