The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
Biology‐Oriented Synthesis
Abstract
Which compound classes are best suited as probes and tools for chemical biology research and as inspiration for medicinal chemistry programs? Chemical space is enormously large and cannot be exploited conclusively by means of synthesis efforts. Methods are required that allow one to identify and map the biologically relevant subspaces of vast chemical space, and serve as hypothesis‐generating tools for inspiring synthesis programs. Biology‐oriented synthesis builds on structural conservatism in the evolution of proteins and natural products. It employs a hierarchical classification of bioactive compounds according to structural relationships and type of bioactivity, and selects the scaffolds of bioactive molecule classes as starting points for the synthesis of compound collections with focused diversity. Navigation in chemical space is facilitated by Scaffold Hunter, an intuitively accessible and highly interactive software. Small molecules synthesized according to BIOS are enriched in bioactivity. They facilitate the analysis of complex biological phenomena by means of acute perturbation and may serve as novel starting points to inspire drug discovery programs.
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Cites
Natural products as sources of new drugs over the last 25 years
Newman, D. J., & Cragg, G. M. (2007) · Journal of Natural Products · doi:10.1021/np068054v · Cited by 5,517
Diagnosis and complications of Cushing’s syndrome: a consensus statement
Arnaldi, G., Angeli, A., Atkinson, A. B., Bertagna, X., Cavagnini, F., Chrousos, G. P., Fava, G. A., Findling, J. W., Gaillard, R. C., Grossman, A. B., et al. (2003) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2003-030871 · Cited by 1,362
Similarity-based virtual screening using 2D fingerprints
Willett, P. (2006) · Drug Discovery Today · doi:10.1016/j.drudis.2006.10.005 · Cited by 849
Morton, N. M., Paterson, J. M., Masuzaki, H., Holmes, M. C., Staels, B., Fievet, C., Walker, B. R., Flier, J. S., Mullins, J. J., & Seckl, J. R. (2004) · Diabetes · doi:10.2337/diabetes.53.4.931 · Cited by 512
Small molecules: the missing link in the central dogma
Schreiber, S. L. (2005) · Nature Chemical Biology · doi:10.1038/nchembio0705-64 · Cited by 306
Cited by
The re-emergence of natural products for drug discovery in the genomics era
Harvey, A. L., Edrada-Ebel, R., & Quinn, R. J. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4510 · Cited by 2,572
Natural Products for Drug Discovery in the 21st Century: Innovations for Novel Drug Discovery
Thomford, N. E., Senthebane, D. A., Rowe, A., Munro, D., Seele, P., Maroyi, A., & Dzobo, K. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19061578 · Cited by 1,241
Opportunities and challenges in phenotypic drug discovery: an industry perspective
Moffat, J. G., Vincent, F., Lee, J. A., Eder, J., & Prunotto, M. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2017.111 · Cited by 939
Schneider, G. (2018) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2017.232 · Cited by 910
Modulators of Protein–Protein Interactions
Milroy, L.-G., Grossmann, T. N., Hennig, S., Brunsveld, L., & Ottmann, C. (2014) · Chemical Reviews · doi:10.1021/cr400698c · Cited by 497
Metadata
- Authors
- Wetzel, S., Bon, R. S., Kumar, K., & Waldmann, H.
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2011-10-28
- Volume
- 50
- Issue
- 46
- Pages
- 10800-10826
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W2095842646
- Cited by
- 505
- References
- 5
- FWCI
- 33.19
- Type
- journal article
- Language
- en
- Open access
- closed
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