Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates.

Reynisson

doi:10.1039/d1dt03553c

Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates.

Reynisson

Authors

Johannes Reynisson j.reynisson@keele.ac.uk

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
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