Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/10637/10822
Título : New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
Autor : Rangasamy, Loganathan.
Pascual-Teresa Fernández, Beatriz de.
Zapico Rodríguez, José María.
Ramos González, Ana.
Ortín Remón, Irene.
Coderch Boué, Claire.
Materias: Dinámica molecular.Drogas de objetivos múltiples.Multi-target drugs.Dual inhibitors.
Fecha de publicación : 9-jun-2020
Resumen : 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.
Descripción : ACS Medicinal Chemistry Letters, ISSN 1948-5875, 11, 5, 713-719.
URI : http://hdl.handle.net/10637/10822
Derechos: http://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
Otros identificadores : 000000717528
Aparece en las colecciones: Facultad de Farmacia

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