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Emergent synthetic methods for the modular advancement of sp(3)-rich fragments
Fragment-based drug discovery is an important and increasingly reliable technology for the delivery of clinical candidates. Notably, however, sp(3)-rich fragments are a largely untapped resource in molecular discovery, in part due to the lack of general and suitably robust chemical methods available...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8179648/ https://www.ncbi.nlm.nih.gov/pubmed/34168751 http://dx.doi.org/10.1039/d1sc00161b |
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author | Caplin, Max J. Foley, Daniel J. |
author_facet | Caplin, Max J. Foley, Daniel J. |
author_sort | Caplin, Max J. |
collection | PubMed |
description | Fragment-based drug discovery is an important and increasingly reliable technology for the delivery of clinical candidates. Notably, however, sp(3)-rich fragments are a largely untapped resource in molecular discovery, in part due to the lack of general and suitably robust chemical methods available to aid their development into higher affinity lead and drug compounds. This Perspective describes the challenges associated with developing sp(3)-rich fragments, and succinctly highlights recent advances in C(sp(3))–H functionalisations of high potential value towards advancing fragment hits by ‘growing’ functionalised rings and chains from unconventional, carbon-centred vectors. |
format | Online Article Text |
id | pubmed-8179648 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
spelling | pubmed-81796482021-06-23 Emergent synthetic methods for the modular advancement of sp(3)-rich fragments Caplin, Max J. Foley, Daniel J. Chem Sci Chemistry Fragment-based drug discovery is an important and increasingly reliable technology for the delivery of clinical candidates. Notably, however, sp(3)-rich fragments are a largely untapped resource in molecular discovery, in part due to the lack of general and suitably robust chemical methods available to aid their development into higher affinity lead and drug compounds. This Perspective describes the challenges associated with developing sp(3)-rich fragments, and succinctly highlights recent advances in C(sp(3))–H functionalisations of high potential value towards advancing fragment hits by ‘growing’ functionalised rings and chains from unconventional, carbon-centred vectors. The Royal Society of Chemistry 2021-03-02 /pmc/articles/PMC8179648/ /pubmed/34168751 http://dx.doi.org/10.1039/d1sc00161b Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
spellingShingle | Chemistry Caplin, Max J. Foley, Daniel J. Emergent synthetic methods for the modular advancement of sp(3)-rich fragments |
title | Emergent synthetic methods for the modular advancement of sp(3)-rich fragments |
title_full | Emergent synthetic methods for the modular advancement of sp(3)-rich fragments |
title_fullStr | Emergent synthetic methods for the modular advancement of sp(3)-rich fragments |
title_full_unstemmed | Emergent synthetic methods for the modular advancement of sp(3)-rich fragments |
title_short | Emergent synthetic methods for the modular advancement of sp(3)-rich fragments |
title_sort | emergent synthetic methods for the modular advancement of sp(3)-rich fragments |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8179648/ https://www.ncbi.nlm.nih.gov/pubmed/34168751 http://dx.doi.org/10.1039/d1sc00161b |
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