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Design and development of Isatin-triazole hydrazones as potential inhibitors of microtubule affinity-regulating kinase 4 for the therapeutic management of cell proliferation and metastasis
Jamia Millia Islamia, Dept Biosci, New Delhi 110025, India;Jamia Millia Islamia, Dept Chem, New Delhi 110025, India.
Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India;Jamia Millia Islamia, Dept Biotechnol, New Delhi 110025, India.
Jamia Millia Islamia, Ctr Interdisciplinary Res Basic Sci, New Delhi 110025, India.ORCID-id: 0000-0002-8566-0248
Jamia Millia Islamia, Dept Chem, New Delhi 110025, India.
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2019 (engelsk)Inngår i: European Journal of Medicinal Chemistry, ISSN 0223-5234, E-ISSN 1768-3254, Vol. 163, s. 840-852Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]

Microtubule affinity-regulating kinase 4 (MARK4) is a potential drug target as the same is found to be over expressed in several types of cancers. In search of effective MARK4 inhibitors, we have synthesized and characterized Isatin-triazole hydrazones (9a-i) and evaluated their inhibitory potential. Of all the compounds, 9g showed better binding affinity and enzyme inhibition potential in sub micromolar range. Human serum albumin (HSA) binding assay suggested an easy transportation of 9g in blood stream due to its binding affinity. In vitro anticancer studies performed on MCF-7, MDA-MB-435s and HepG2 cells using 9g showed inhibition of cell proliferation and cell migration. Further, 9g induces apoptosis in these cancerous cells, with IC50 values of 6.22, 9.94 and 8.14 mu M, respectively. Putatively, 9g seems to cause oxidative stress resulting in apoptosis. Functional assay of 9g with a panel of 26 kinases showed MARK4 specific profile. In conclusion, 9g seems to possess an effective inhibitory potential towards MARK4 adding an additional repertoire to anticancer therapeutics.

sted, utgiver, år, opplag, sider
2019. Vol. 163, s. 840-852
Emneord [en]
Microtubule affinity-regulating kinase 4, Isatin-triazole hydrazones, Cell proliferation, Oxidative stress, Apoptosis, Metastasis
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Identifikatorer
URN: urn:nbn:se:uu:diva-378190DOI: 10.1016/j.ejmech.2018.12.026ISI: 000458597300061PubMedID: 30579124OAI: oai:DiVA.org:uu-378190DiVA, id: diva2:1293228
Tilgjengelig fra: 2019-03-04 Laget: 2019-03-04 Sist oppdatert: 2019-03-04bibliografisk kontrollert

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