Rangasamy, LoganathanRamos González, Ana MaríaCoderch Boué, ClairePascual-Teresa Fernández, Beatriz deZapico Rodríguez, José MaríaOrtín Remón, Irene2020-06-092020-06-092020-06-09http://hdl.handle.net/10637/10822ACS Medicinal Chemistry Letters, ISSN 1948-5875, 2020, 11, 5, 713-719.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.application/pdfenopen accessDinámica molecular.Drogas de objetivos múltiples.Multi-target drugs.Dual inhibitors.Artículo10.1021/acsmedchemlett.9b00561https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es