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Discovery of selective, antimetastatic and anti-cancer stem cell metallohelices via post-assembly modification
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Song, Hualong, Rogers, Nicola J., Allison, Simon J., Brabec, Viktor, Bridgewater, Hannah, Kostrhunova, Hana, Markova, Lenka, Phillips, Roger M., Pinder, Emma C., Shepherd, Samantha L., Young, Lawrence S., Zajac, Juraj and Scott, Peter (2019) Discovery of selective, antimetastatic and anti-cancer stem cell metallohelices via post-assembly modification. Chemical Science, 10 (37). pp. 8547-8557. doi:10.1039/C9SC02651G ISSN 2041-6520.
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Official URL: http://dx.doi.org/10.1039/C9SC02651G
Abstract
Helicates and related metallofoldamers, synthesised by dynamic self-assembly, represent an area of chemical space inaccessible by traditional organic synthesis, and yet with potential for discovery of new classes of drug. Here we report that water-soluble, optically pure Fe(II)- and even Zn(II)-based triplex metallohelices are an excellent platform for post-assembly click reactions. By these means, the in vitro anticancer activity and most importantly the selectivity of a triplex metallohelix Fe(II) system are dramatically improved. For one compound, a remarkable array of mechanistic and pharmacological behaviours is discovered: inhibition of Na+/K+ ATPase with potency comparable to the drug ouabain, antimetastatic properties (including inhibition of cell migration, re-adhesion and invasion), cancer stem cell targeting, and finally colonosphere inhibition competitive with the drug salinomycin.
Item Type: | Journal Article | |||||||||||||||||||||
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Subjects: | Q Science > QD Chemistry | |||||||||||||||||||||
Divisions: | Faculty of Science, Engineering and Medicine > Science > Chemistry Faculty of Science, Engineering and Medicine > Medicine > Warwick Medical School |
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Library of Congress Subject Headings (LCSH): | Metallofoldamers, Supramolecular chemistry, Cancer cells, Stem cells -- Research, Drug resistance in cancer cells | |||||||||||||||||||||
Journal or Publication Title: | Chemical Science | |||||||||||||||||||||
Publisher: | Royal Society of Chemistry | |||||||||||||||||||||
ISSN: | 2041-6520 | |||||||||||||||||||||
Official Date: | 18 July 2019 | |||||||||||||||||||||
Dates: |
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Volume: | 10 | |||||||||||||||||||||
Number: | 37 | |||||||||||||||||||||
Page Range: | pp. 8547-8557 | |||||||||||||||||||||
DOI: | 10.1039/C9SC02651G | |||||||||||||||||||||
Status: | Peer Reviewed | |||||||||||||||||||||
Publication Status: | Published | |||||||||||||||||||||
Access rights to Published version: | Open Access (Creative Commons) | |||||||||||||||||||||
Date of first compliant deposit: | 12 August 2019 | |||||||||||||||||||||
Date of first compliant Open Access: | 14 August 2019 | |||||||||||||||||||||
RIOXX Funder/Project Grant: |
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