New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.

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dc.centroUniversidad San Pablo-CEU
dc.contributor.authorRangasamy, Loganathan
dc.contributor.authorRamos González, Ana María
dc.contributor.authorCoderch Boué, Claire
dc.contributor.authorPascual-Teresa Fernández, Beatriz de
dc.contributor.authorZapico Rodríguez, José María
dc.contributor.authorOrtín Remón, Irene
dc.date2020
dc.date.accessioned2020-06-09T04:00:17Z
dc.date.available2020-06-09T04:00:17Z
dc.date.issued2020-06-09
dc.descriptionACS Medicinal Chemistry Letters, ISSN 1948-5875, 2020, 11, 5, 713-719.
dc.description.abstractFour 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.en
dc.description.versionPost-printen
dc.formatapplication/pdf
dc.identifier000000717528
dc.identifier.doi10.1021/acsmedchemlett.9b00561
dc.identifier.urihttp://hdl.handle.net/10637/10822
dc.language.isoen
dc.relationFinanciado con cargo a proyectos del Ministerio (MICIU/FEDER, UE grant number RTI2018-093539-B-I00) y de la Unión Europea (European Union?s Horizon 2020 research and innovation pro-gramme under the Marie-Sklodowska-Curie grant agreement number DUALITY 746225).es
dc.rightsopen access
dc.rights.cchttps://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subjectDinámica molecular.
dc.subjectDrogas de objetivos múltiples.es
dc.subjectMulti-target drugs.en
dc.subjectDual inhibitors.en
dc.titleNew Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
dc.typeArtículo
dspace.entity.typePublicationes
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relation.isAuthorOfPublication.latestForDiscoveryac3c2128-fa85-4881-a056-bbeb0e359a4b

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