Please use this identifier to cite or link to this item: http://hdl.handle.net/10637/10822

New 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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