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Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile
Here we describe a rapid and divergent synthetic route toward structurally novel αHTs functionalized with either one or two thioether or sulfonyl appendages. Evaluation of this library against hepatitis B and herpes simplex virus, as well as the pathogenic fungus Cryptococcus neoformans, revealed co...
| Autores principales: | , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
The Royal Society of Chemistry
2019
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7543996/ https://www.ncbi.nlm.nih.gov/pubmed/33042521 http://dx.doi.org/10.1039/c9ra06383h |
| _version_ | 1783591767773282304 |
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| author | Agyemang, Nana B. Kukla, Cassandra R. Edwards, Tiffany C. Li, Qilan Langen, Madison K. Schaal, Alexandra Franson, Abaigeal D. Casals, Andreu Gazquez Donald, Katherine A. Yu, Alice J. Donlin, Maureen J. Morrison, Lynda A. Tavis, John E. Murelli, Ryan P. |
| author_facet | Agyemang, Nana B. Kukla, Cassandra R. Edwards, Tiffany C. Li, Qilan Langen, Madison K. Schaal, Alexandra Franson, Abaigeal D. Casals, Andreu Gazquez Donald, Katherine A. Yu, Alice J. Donlin, Maureen J. Morrison, Lynda A. Tavis, John E. Murelli, Ryan P. |
| author_sort | Agyemang, Nana B. |
| collection | PubMed |
| description | Here we describe a rapid and divergent synthetic route toward structurally novel αHTs functionalized with either one or two thioether or sulfonyl appendages. Evaluation of this library against hepatitis B and herpes simplex virus, as well as the pathogenic fungus Cryptococcus neoformans, revealed complementary biological profiles and new lead compounds with sub-micromolar activities against each pathogen and high selectivities when compared to mammalian cell lines. |
| format | Online Article Text |
| id | pubmed-7543996 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2019 |
| publisher | The Royal Society of Chemistry |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-75439962020-10-08 Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile Agyemang, Nana B. Kukla, Cassandra R. Edwards, Tiffany C. Li, Qilan Langen, Madison K. Schaal, Alexandra Franson, Abaigeal D. Casals, Andreu Gazquez Donald, Katherine A. Yu, Alice J. Donlin, Maureen J. Morrison, Lynda A. Tavis, John E. Murelli, Ryan P. RSC Adv Chemistry Here we describe a rapid and divergent synthetic route toward structurally novel αHTs functionalized with either one or two thioether or sulfonyl appendages. Evaluation of this library against hepatitis B and herpes simplex virus, as well as the pathogenic fungus Cryptococcus neoformans, revealed complementary biological profiles and new lead compounds with sub-micromolar activities against each pathogen and high selectivities when compared to mammalian cell lines. The Royal Society of Chemistry 2019-10-23 /pmc/articles/PMC7543996/ /pubmed/33042521 http://dx.doi.org/10.1039/c9ra06383h Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
| spellingShingle | Chemistry Agyemang, Nana B. Kukla, Cassandra R. Edwards, Tiffany C. Li, Qilan Langen, Madison K. Schaal, Alexandra Franson, Abaigeal D. Casals, Andreu Gazquez Donald, Katherine A. Yu, Alice J. Donlin, Maureen J. Morrison, Lynda A. Tavis, John E. Murelli, Ryan P. Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile |
| title | Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile |
| title_full | Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile |
| title_fullStr | Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile |
| title_full_unstemmed | Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile |
| title_short | Divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile |
| title_sort | divergent synthesis of a thiolate-based α-hydroxytropolone library with a dynamic bioactivity profile |
| topic | Chemistry |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7543996/ https://www.ncbi.nlm.nih.gov/pubmed/33042521 http://dx.doi.org/10.1039/c9ra06383h |
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