biostudies-literaturePeerzada MNScience and Engineering Research BoardCouncil of Scientific and Industrial ResearchIndian Council of Medical ResearchDepartment of Biotechnology , Ministry of Science and Technology22759-22771https://www.ebi.ac.uk/biostudies/studies/S-EPMC7495461biostudies-literatureUnknown5(36)Microtubule affinity-regulating kinase 4 (MARK4), a member of the serine/threonine kinase family, is an emerging therapeutic target in anticancer drug discovery paradigm due to its involvement in regulation of microtubule dynamics, cell cycle regulation, and cancer progression. Therefore, to identify the novel chemical architecture for the design and development of novel MARK4 inhibitors with concomitant radical scavenging property, a series of small-molecule arylaldoxime/5-nitroimidazole conjugates were designed and synthesized via multistep chemical reactions following the pharmacophoric hybridization approach. Compound <b>4h</b> was identified as a promising MARK4 inhibitor with high selectivity toward MARK4 inhibition as compared to the panel of screened <b>30</b> kinases pertaining toACS omegaDesign and Development of Small-Molecule Arylaldoxime/5-Nitroimidazole Hybrids as Potent Inhibitors of MARK4: A Promising Approach for Target-Based Cancer Therapy.PMC749546145/9/2019-PHA/BMSBT/PR12828/AAQ/1/622/201509/466 (0220) 2K19 EMR-IEMR/2015/002372Avecilla FSiddiqui SMHassan MIPeerzada MNKhan PAzam AKhan NSfalseDesign and Development of Small-Molecule Arylaldoxime/5-Nitroimidazole Hybrids as Potent Inhibitors of MARK4: A Promising Approach for Target-Based Cancer Therapy.Microtubule affinity-regulating kinase 4 (MARK4), a member of the serine/threonine kinase family, is an emerging therapeutic target in anticancer drug discovery paradigm due to its involvement in regulation of microtubule dynamics, cell cycle regulation, and cancer progression. Therefore, to identify the novel chemical architecture for the design and development of novel MARK4 inhibitors with concomitant radical scavenging property, a series of small-molecule arylaldoxime/5-nitroimidazole conjugates were designed and synthesized via multistep chemical reactions following the pharmacophoric hybridization approach. Compound <b>4h</b> was identified as a promising MARK4 inhibitor with high selectivity toward MARK4 inhibition as compared to the panel of screened <b>30</b> kinases pertaining to2020-01-01T00:00:00Z2020 Sep2026-05-08T20:19:28.735Z2020-09-25T07:02:26ZS-EPMC74954613295412310.1021/acsomega.0c01703