Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases
The cell division cycle 25 phosphatases (CDC25A, B, and C; E.C. 3.1.3.48) are key regulator of the cell cycle in human cells. Their aberrant expression has been associated with the insurgence and development of various types of cancer, and with a poor clinical prognosis. Therefore, CDC25 phosphatase...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2017-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/14756366.2016.1238364 |
| _version_ | 1818502992911925248 |
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| author | Emilie Evain-Bana Lucie Schiavo Christophe Bour Don Antoine Lanfranchi Simone Berardozzi Francesca Ghirga Denyse Bagrel Bruno Botta Gilles Hanquet Mattia Mori |
| author_facet | Emilie Evain-Bana Lucie Schiavo Christophe Bour Don Antoine Lanfranchi Simone Berardozzi Francesca Ghirga Denyse Bagrel Bruno Botta Gilles Hanquet Mattia Mori |
| author_sort | Emilie Evain-Bana |
| collection | DOAJ |
| description | The cell division cycle 25 phosphatases (CDC25A, B, and C; E.C. 3.1.3.48) are key regulator of the cell cycle in human cells. Their aberrant expression has been associated with the insurgence and development of various types of cancer, and with a poor clinical prognosis. Therefore, CDC25 phosphatases are a valuable target for the development of small molecule inhibitors of therapeutic relevance. Here, we used an integrated strategy mixing organic chemistry with biological investigation and molecular modeling to study novel quinonoid derivatives as CDC25 inhibitors. The most promising molecules proved to inhibit CDC25 isoforms at single digit micromolar concentration, becoming valuable tools in chemical biology investigations and profitable leads for further optimization. |
| first_indexed | 2024-12-10T21:17:46Z |
| format | Article |
| id | doaj.art-9849d8058a8e460d947b419399a0e753 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-12-10T21:17:46Z |
| publishDate | 2017-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-9849d8058a8e460d947b419399a0e7532022-12-22T01:33:14ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742017-01-0132111311810.1080/14756366.2016.12383641238364Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatasesEmilie Evain-Bana0Lucie Schiavo1Christophe Bour2Don Antoine Lanfranchi3Simone Berardozzi4Francesca Ghirga5Denyse Bagrel6Bruno Botta7Gilles Hanquet8Mattia Mori9Université de LorraineUniversité de StrasbourgUniversitéUniversité de StrasbourgSapienza University of RomaCenter for Life Nano Science@SapienzaUniversité de LorraineSapienza University of RomaUniversité de StrasbourgCenter for Life Nano Science@SapienzaThe cell division cycle 25 phosphatases (CDC25A, B, and C; E.C. 3.1.3.48) are key regulator of the cell cycle in human cells. Their aberrant expression has been associated with the insurgence and development of various types of cancer, and with a poor clinical prognosis. Therefore, CDC25 phosphatases are a valuable target for the development of small molecule inhibitors of therapeutic relevance. Here, we used an integrated strategy mixing organic chemistry with biological investigation and molecular modeling to study novel quinonoid derivatives as CDC25 inhibitors. The most promising molecules proved to inhibit CDC25 isoforms at single digit micromolar concentration, becoming valuable tools in chemical biology investigations and profitable leads for further optimization.http://dx.doi.org/10.1080/14756366.2016.1238364CDC25enzyme inhibitorsquinonoidorganic synthesismolecular modeling |
| spellingShingle | Emilie Evain-Bana Lucie Schiavo Christophe Bour Don Antoine Lanfranchi Simone Berardozzi Francesca Ghirga Denyse Bagrel Bruno Botta Gilles Hanquet Mattia Mori Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases Journal of Enzyme Inhibition and Medicinal Chemistry CDC25 enzyme inhibitors quinonoid organic synthesis molecular modeling |
| title | Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases |
| title_full | Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases |
| title_fullStr | Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases |
| title_full_unstemmed | Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases |
| title_short | Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases |
| title_sort | synthesis biological evaluation and molecular modeling studies on novel quinonoid inhibitors of cdc25 phosphatases |
| topic | CDC25 enzyme inhibitors quinonoid organic synthesis molecular modeling |
| url | http://dx.doi.org/10.1080/14756366.2016.1238364 |
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