The DOI matches its Crossref record; 49 of the 49 references it cites were found in a registry or an index.
Lead‐Oriented Synthesis: A New Opportunity for Synthetic Chemistry
Abstract
The pharmaceutical industry remains solely reliant on synthetic chemistry methodology to prepare compounds for small‐molecule drug discovery programmes. The importance of the physicochemical properties of these molecules in determining their success in drug development is now well understood but we present here data suggesting that much synthetic methodology is unintentionally predisposed to producing molecules with poorer drug‐like properties. This bias may have ramifications to the early hit‐ and lead‐finding phases of the drug discovery process when larger numbers of compounds from array techniques are prepared. To address this issue we describe for the first time the concept of lead‐oriented synthesis and the opportunity for its adoption to increase the range and quality of molecules used to develop new medicines.
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Cites
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Can the pharmaceutical industry reduce attrition rates?
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Target-Oriented and Diversity-Oriented Organic Synthesis in Drug Discovery
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The influence of drug-like concepts on decision-making in medicinal chemistry
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A ‘Rule of Three’ for fragment-based lead discovery?
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Generation of a Set of Simple, Interpretable ADMET Rules of Thumb
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Cited by
The medicinal chemist's toolbox for late stage functionalization of drug-like molecules
Cernak, T., Dykstra, K. D., Tyagarajan, S., Vachal, P., & Krska, S. W. (2016) · Chemical Society Reviews · doi:10.1039/c5cs00628g · Cited by 1,743
Expanding the medicinal chemistry synthetic toolbox
Boström, J., Brown, D. G., Young, R. J., & Keserü, G. M. (2018) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2018.116 · Cited by 665
Finding the sweet spot: the role of nature and nurture in medicinal chemistry
Hann, M. M., & Keserü, G. M. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3701 · Cited by 411
The Necessary Nitrogen Atom: A Versatile High-Impact Design Element for Multiparameter Optimization
Pennington, L. D., & Moustakas, D. T. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01807 · Cited by 408
Cross-Electrophile Coupling: Principles, Methods, and Applications in Synthesis
Ehehalt, L. E., Beleh, O. M., Priest, I. C., Mouat, J. M., Olszewski, A. K., Ahern, B. N., Cruz, A. R., Chi, B. K., Castro, A. J., Kang, K., et al. (2024) · Chemical Reviews · doi:10.1021/acs.chemrev.4c00524 · Cited by 312
Metadata
- Authors
- Nadin, A., Hattotuwagama, C., & Churcher, I.
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2012-01-03
- Volume
- 51
- Issue
- 5
- Pages
- 1114-1122
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W1975237431
- Cited by
- 390
- References
- 49
- FWCI
- 36.99
- Type
- journal article
- Language
- en
- Open access
- closed
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- Nadin, A., Hattotuwagama, C., & Churcher, I. (2012). Lead‐Oriented Synthesis: A New Opportunity for Synthetic Chemistry. Angewandte Chemie International Edition. https://doi.org/10.1002/anie.201105840
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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