Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/106352
Title: Screening of ferrocenyl–phosphines identifies a gold-coordinated derivative as a novel anticancer agent for hematological malignancies
Authors: Verma, Navin Kumar
Sadeer, Abdul
Kizhakeyil, Atish
Pang, Jia Hao
Tay, Shan Wen
Kumar, Pankaj
Chiu, Angela Qi Yun
Pullarkat, Sumod Appukuttan
Keywords: Science::Chemistry
Hematological Malignancies
Anticancer Agents
Issue Date: 2018
Source: Verma, 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/C8RA05224G
Series/Report no.: RSC Advances
Abstract: The 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.
URI: https://hdl.handle.net/10356/106352
http://hdl.handle.net/10220/49584
DOI: 10.1039/C8RA05224G
Rights: © 2018 The Royal Society of Chemistry. This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:LKCMedicine Journal Articles

Google ScholarTM

Check

Altmetric


Plumx

Items in DR-NTU are protected by copyright, with all rights reserved, unless otherwise indicated.