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Inhibition of CK2 and PIM-1 kinase activity has been shown to significantly reduce the viability of cancer cells by inducing apoptosis. A series of novel amino alcohol derivatives of parental DMAT were designed and synthesized as potent dual CK2\/PIM-1 inhibitors. Concomitantly with the inhibition studies toward recombinant CK2 and PIM-1, the influence of the obtained compounds on the viability of three human carcinoma cell lines, i.e., acute lymphoblastic leukemia (CCRF-CEM), human chronic myelogenous leukemia (K-562), and breast cancer (MCF-7), as well as non-cancerous cells (Vero), was evaluated using an MTT assay. Induction of apoptosis and cell cycle progression after treatment with the most active compound and a lead compound were studied by flow-cytometry-based assay. Additionally, autophagy induction in K-562 cells and intracellular inhibition of CK2 and PIM-1 in all the tested cell lines were evaluated by qualitative\/quantitative fluorescence-based assay and Western blot method, respectively. Among the newly developed inhibitors, 1,1,1-trifluoro-3-[(4,5,6,7-tetrabromo-1H-benzimidazol-2-yl)amino]propan-2-ol demonstrates the highest selectivity and the most prominent proapoptotic properties towards the studied cancer cells, especially towards acute lymphoblastic leukemia, in addition to inducing autophagy in K-562 cells.<\/jats:p>","DOI":"10.3390\/pharmaceutics15071991","type":"journal-article","created":{"date-parts":[[2023,7,21]],"date-time":"2023-07-21T01:52:35Z","timestamp":1689904355000},"page":"1991","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":17,"title":["Synthesis and Anticancer Activity of Novel Dual Inhibitors of Human Protein Kinases CK2 and PIM-1"],"prefix":"10.3390","volume":"15","author":[{"given":"Patrycja","family":"Wi\u0144ska","sequence":"first","affiliation":[{"name":"Faculty of Chemistry, Warsaw University of Technology, 00-664 Warsaw, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Monika","family":"Wielechowska","sequence":"additional","affiliation":[{"name":"Faculty of Chemistry, Warsaw University of Technology, 00-664 Warsaw, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Miros\u0142awa","family":"Koronkiewicz","sequence":"additional","affiliation":[{"name":"Department of Biomedical Research, National Medicines Institute, 00-725 Warsaw, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5355-7281","authenticated-orcid":false,"given":"Pawe\u0142","family":"Borowiecki","sequence":"additional","affiliation":[{"name":"Faculty of Chemistry, Warsaw University of Technology, 00-664 Warsaw, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2023,7,20]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"899","DOI":"10.1007\/s11010-022-04558-2","article-title":"Protein kinase CK2\u2014Diverse roles in cancer cell biology and therapeutic promise","volume":"478","author":"Trembley","year":"2023","journal-title":"Mol. 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