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dc.contributor.authorPeerzada, Mudasir Nabi
dc.contributor.authorKhan, Parvez
dc.contributor.authorKhan, Nashrah Sharif
dc.contributor.authorAvecilla, Fernando
dc.contributor.authorSiddiqui, Shadab Miyan
dc.contributor.authorHassan, Imtaiyaz
dc.contributor.authorAzam, Amir
dc.date.accessioned2020-10-29T16:07:04Z
dc.date.available2020-10-29T16:07:04Z
dc.date.issued2020-09-01
dc.identifier.citationPeerzada, M. N.; Khan, P.; Khan, N. S.; Avecilla, F.; Siddiqui, S. M.; Hassan, M. I.; Azam, A. Design and Development of Small-Molecule Arylaldoxime/5-Nitroimidazole Hybrids as Potent Inhibitors of MARK4: A Promising Approach for Target-Based Cancer Therapy. ACS Omega 2020, 5 (36), 22759–22771. https://doi.org/10.1021/acsomega.0c01703.es_ES
dc.identifier.issn2470-1343
dc.identifier.urihttp://hdl.handle.net/2183/26590
dc.description.abstract[Abstract] 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 4h was identified as a promising MARK4 inhibitor with high selectivity toward MARK4 inhibition as compared to the panel of screened 30 kinases pertaining to the serine/threonine family, which was validated by molecular docking and fluorescence binding studies. The comprehensive cell-based examination divulged the promising apoptotic, antiproliferative, and antioxidant potential for the chemotype 4h. The compound 4h was endowed with the Ka value of 3.6 × 103 M–1 for human serum albumin, which reflects its remarkable transportation and delivery properties to the target site via blood. The present study impedes that in the future, such compounds may stand as optimized pharmacological lead candidates in drug discovery for targeting cancer via MARK4 inhibition with a remarkable anticancer profile.es_ES
dc.description.sponsorshipCouncil of Scientific and Industrial Research (India); 09/466 (0220) 2K19 EMR-Ies_ES
dc.description.sponsorshipGovernment of India; EMR/2015/002372es_ES
dc.description.sponsorshipGovernment of India; BT/PR12828/AAQ/1/622/2015es_ES
dc.description.sponsorshipIndian Council of Medical Research; 45/9/2019-PHA/BMSes_ES
dc.language.isoenges_ES
dc.publisherAmerican Chemical Societyes_ES
dc.relation.urihttps://doi.org/10.1021/acsomega.0c01703es_ES
dc.rightsAtribución-NoComercial-SinDerivadas 4.0 Españaes_ES
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/es/*
dc.titleDesign and Development of Small-Molecule Arylaldoxime/5-Nitroimidazole Hybrids as Potent Inhibitors of MARK4: a Promising Approach for Target-Based Cancer Therapyes_ES
dc.typeinfo:eu-repo/semantics/articlees_ES
dc.rights.accessinfo:eu-repo/semantics/openAccesses_ES
UDC.journalTitleACS Omegaes_ES
UDC.volume5es_ES
UDC.issue36es_ES
UDC.startPage22759es_ES
UDC.endPage22771es_ES


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