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http://hdl.handle.net/10637/10822New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
| Title: | New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. |
| Authors : | Rangasamy, Loganathan Pascual-Teresa Fernández, Beatriz de Zapico Rodríguez, José María Ramos González, Ana Ortín Remón, Irene Coderch Boué, Claire |
| Keywords: | Dinámica molecular.; Drogas de objetivos múltiples.; Multi-target drugs.; Dual inhibitors. |
| Abstract: | Four potent CK2 inhibitors derived from CX-4945 are described. They are provided also of nanomolar activity against HDAC1, therefore having promising utility as dual-target agents for cancer. The linker length between the hydroxamic acid and the CX-4945 scaffold plays an important role in dictating balanced activity against the targeted enzymes. The seven-carbon linker (compound 15c) was optimal for inhibition of both CK2 and HDAC1. Remarkably, 15c showed 3.0 and 3.5 times higher inhibitory activity than the reference compounds CX-4945 (against CK2) and SAHA (against HDAC1), respectively. Compound 15c exhibited micromolar activity in cell-based cytotoxic assays against multiple cell lines. |
| Description: | ACS Medicinal Chemistry Letters, ISSN 1948-5875, 2020, 11, 5, 713-719. |
| URI: | http://hdl.handle.net/10637/10822 |
| Rights : | http://creativecommons.org/licenses/by-nc-nd/4.0/deed.es |
| Issue Date: | 9-Jun-2020 |
| Center : | Universidad San Pablo-CEU |
| Appears in Collections: | Facultad de Farmacia |
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