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Cited by 505

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Biology‐Oriented Synthesis

Wetzel, Stefan, Bon, Robin S., Kumar, Kamal, Waldmann, Herbert·2011·Angewandte Chemie International Edition

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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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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CoChat. (2026). Citation check: Biology‐Oriented Synthesis. https://app.cochat.ai/papers/10.1002/anie.201007004
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Wetzel, S., Bon, R. S., Kumar, K., & Waldmann, H. (2011). Biology‐Oriented Synthesis. Angewandte Chemie International Edition. https://doi.org/10.1002/anie.201007004

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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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