Johannes Reynisson j.reynisson@keele.ac.uk
Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates.
Reynisson
Authors
Abstract
The incorporation of the ferrocenyl moiety into a bioactive molecule may significantly alter the activity of the resulting conjugate. By applying this strategy, we designed ferrocenyl analogs of monastrol - the first low molecular weight kinesin spindle protein (KSP) inhibitor. The obtained compounds showed low micromolar antiproliferative activity towards a panel of sensitive and ABC-overexpressing cancer cells. Most cytotoxic compounds exhibited also higher KSP modulatory activity and ability for ROS generation compared to monastrol. The increased bioactivity of the studied compounds can be attributed to the presence of the ferrocenyl group.
Acceptance Date | Nov 11, 2021 |
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Publication Date | Nov 17, 2021 |
Journal | Dalton Transactions |
Print ISSN | 1477-9226 |
Publisher | Royal Society of Chemistry |
DOI | https://doi.org/10.1039/d1dt03553c |
Publisher URL | https://pubs.rsc.org/en/content/articlelanding/2021/DT/D1DT03553C |
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Manuscript_ACS_20210930 CH-JR.docx
(2 Mb)
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Publisher Licence URL
https://creativecommons.org/licenses/by-nc/4.0/
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