dc.contributor.authorVerma, Navin Kumar
dc.contributor.authorSadeer, Abdul
dc.contributor.authorKizhakeyil, Atish
dc.contributor.authorPang, Jia Hao
dc.contributor.authorChiu, Angela Qi Yun
dc.contributor.authorTay, Shan Wen
dc.contributor.authorKumar, Pankaj
dc.contributor.authorPullarkat, Sumod Appukuttan
dc.identifier.citationVerma, N. K., Sadeer, A., Kizhakeyil, A., Pang, J. H., Chiu, A. Q. Y., Tay, S. W., . . . Pullarkat, S. A. (2018). Screening of ferrocenyl–phosphines identifies a gold-coordinated derivative as a novel anticancer agent for hematological malignancies. RSC Advances, 8(51), 28960-28968. doi:10.1039/C8RA05224Gen_US
dc.description.abstractThe development of new organometallic compounds as anticancer agents is currently an active area of research. Here, we report the design, synthesis and characterization of a panel of 10 new ferrocenyl–phosphine derivatives (FD1–FD10) and the analysis of their anti-proliferative activities in hematolymphoid cells representing non-Hodgkin cutaneous T-cell lymphoma (CTCL). The gold-coordinated ferrocenyl–phosphine complex FD10 exhibited a significant and dose-dependent cytotoxicity in 4 different CTCL cell lines – HuT78, HH, MJ and MyLa. FD10 concentrations causing 50% cell growth inhibition (IC50) of HuT78, HH, MJ and MyLa cells at 24 h were recorded to be 5.55 ± 0.20, 7.80 ± 0.09, 3.16 ± 0.10 and 6.46 ± 0.24 μM respectively. Further mechanistic studies showed that FD10 induced apoptosis in CTCL cells by an intrinsic pathway mediated via the activation of caspase-3 and poly(ADP-ribose)polymerase. It suppressed the expression and activity of STAT3 oncoprotein in CTCL cells. FD10 caused robust G0/G1 phase cell cycle arrest and reduced the expression levels of Akt S473 phosphorylation and c-Myc, both are key cell cycle regulator proteins. Taken together, this study highlights anticancer properties of the ferrocenyl–phosphine gold organometallic complex FD10 and suggests that further development of this novel class of molecule may contribute to new drug discovery for certain hematolymphoid malignancies.en_US
dc.description.sponsorshipMOE (Min. of Education, S’pore)en_US
dc.format.extent9 p.en_US
dc.relation.ispartofseriesRSC Advancesen_US
dc.rights© 2018 The Royal Society of Chemistry. This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.en_US
dc.subjectHematological Malignanciesen_US
dc.subjectAnticancer Agentsen_US
dc.titleScreening of ferrocenyl–phosphines identifies a gold-coordinated derivative as a novel anticancer agent for hematological malignanciesen_US
dc.typeJournal Article
dc.contributor.schoolSchool of Physical and Mathematical Sciencesen_US
dc.contributor.schoolLee Kong Chian School of Medicine (LKCMedicine)en_US
dc.description.versionPublished versionen_US

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