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Inorganics 2017, 5(1), 12; doi:10.3390/inorganics5010012

A Cancer Stem Cell Potent Cobalt(III)–Cyclam Complex Bearing Two Tolfenamic Acid Moieties

Department of Chemistry, King’s College London, London SE1 1DB, UK
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Author to whom correspondence should be addressed.
Academic Editor: Luigi Messori
Received: 19 December 2016 / Revised: 17 January 2017 / Accepted: 25 January 2017 / Published: 9 February 2017
(This article belongs to the Special Issue Tumor Inhibiting Metal Complexes)
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Abstract

Cancer stem cells (CSCs) are thought to be responsible for cancer relapse. CSCs are a subtype of cancer cells with the ability to differentiate, self-renew, and form secondary or tertiary tumors. Current cancer treatments—including chemotherapy, radiation, and surgery—effectively remove bulk cancer cells but are unable to eliminate CSCs. Here, we present the synthesis, characterization, and anti-CSC properties of a cobalt(III)–cyclam complex bearing two tolfenamic acid moieties, 3. Notably, 3 displays sub-micromolar potency towards breast CSCs and bulk breast cancer cells. Detailed mechanistic studies show that 3 is taken up readily by breast CSCs, enters the nucleus, causes DNA damage, and induces caspase-dependent apoptosis. Furthermore, 3 inhibits cyclooxygenase-2 (COX-2) expression in CSCs. The mechanism of action of 3 is similar to that of a naproxen-appended cobalt(III)–cyclam complex, 1 recently reported by our group. The advantage of 3 over 1 is that it has the potential to remove whole tumor populations (bulk cancer cells and CSCs) with a single dose. View Full-Text
Keywords: metallopharmaceuticals; cobalt(III)–cyclam complexes; cancer stem cell; nonsteroidal anti-inflammatory drug; DNA damage; COX-2 inhibition metallopharmaceuticals; cobalt(III)–cyclam complexes; cancer stem cell; nonsteroidal anti-inflammatory drug; DNA damage; COX-2 inhibition
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Cressey, P.B.; Eskandari, A.; Suntharalingam, K. A Cancer Stem Cell Potent Cobalt(III)–Cyclam Complex Bearing Two Tolfenamic Acid Moieties. Inorganics 2017, 5, 12.

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