Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections
Fragment-based drug discovery (FBDD) is a well-established approach for the discovery of novel medicines, illustrated by the approval of two FBBD-derived drugs. This methodology is based on the utilization of small “fragment” molecules (<300 Da) as starting points for drug discovery and optim...
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Frontiers Media S.A.
2018-10-01
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| Series: | Frontiers in Chemistry |
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| Online Access: | https://www.frontiersin.org/article/10.3389/fchem.2018.00460/full |
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doaj-68637d144f844d92bc3f7ab39b34ca7d2020-11-25T00:08:39ZengFrontiers Media S.A.Frontiers in Chemistry2296-26462018-10-01610.3389/fchem.2018.00460411464Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment CollectionsSarah L. KiddThomas J. OsbergerNatalia MateuHannah F. SoreDavid R. SpringFragment-based drug discovery (FBDD) is a well-established approach for the discovery of novel medicines, illustrated by the approval of two FBBD-derived drugs. This methodology is based on the utilization of small “fragment” molecules (<300 Da) as starting points for drug discovery and optimization. Organic synthesis has been identified as a significant obstacle in FBDD, however, in particular owing to the lack of novel 3-dimensional (3D) fragment collections that feature useful synthetic vectors for modification of hit compounds. Diversity-oriented synthesis (DOS) is a synthetic strategy that aims to efficiently produce compound collections with high levels of structural diversity and three-dimensionality and is therefore well-suited for the construction of novel fragment collections. This Mini-Review highlights recent studies at the intersection of DOS and FBDD aiming to produce novel libraries of diverse, polycyclic, fragment-like compounds, and their application in fragment-based screening projects.https://www.frontiersin.org/article/10.3389/fchem.2018.00460/fullfragment-based drug discoverydiversity-oriented synthesismedicinal chemistryorganic synthesiscompound collections |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Sarah L. Kidd Thomas J. Osberger Natalia Mateu Hannah F. Sore David R. Spring |
| spellingShingle |
Sarah L. Kidd Thomas J. Osberger Natalia Mateu Hannah F. Sore David R. Spring Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections Frontiers in Chemistry fragment-based drug discovery diversity-oriented synthesis medicinal chemistry organic synthesis compound collections |
| author_facet |
Sarah L. Kidd Thomas J. Osberger Natalia Mateu Hannah F. Sore David R. Spring |
| author_sort |
Sarah L. Kidd |
| title |
Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections |
| title_short |
Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections |
| title_full |
Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections |
| title_fullStr |
Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections |
| title_full_unstemmed |
Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections |
| title_sort |
recent applications of diversity-oriented synthesis toward novel, 3-dimensional fragment collections |
| publisher |
Frontiers Media S.A. |
| series |
Frontiers in Chemistry |
| issn |
2296-2646 |
| publishDate |
2018-10-01 |
| description |
Fragment-based drug discovery (FBDD) is a well-established approach for the discovery of novel medicines, illustrated by the approval of two FBBD-derived drugs. This methodology is based on the utilization of small “fragment” molecules (<300 Da) as starting points for drug discovery and optimization. Organic synthesis has been identified as a significant obstacle in FBDD, however, in particular owing to the lack of novel 3-dimensional (3D) fragment collections that feature useful synthetic vectors for modification of hit compounds. Diversity-oriented synthesis (DOS) is a synthetic strategy that aims to efficiently produce compound collections with high levels of structural diversity and three-dimensionality and is therefore well-suited for the construction of novel fragment collections. This Mini-Review highlights recent studies at the intersection of DOS and FBDD aiming to produce novel libraries of diverse, polycyclic, fragment-like compounds, and their application in fragment-based screening projects. |
| topic |
fragment-based drug discovery diversity-oriented synthesis medicinal chemistry organic synthesis compound collections |
| url |
https://www.frontiersin.org/article/10.3389/fchem.2018.00460/full |
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