Wieczorek-Błauż, A, Kowalczyk, K, Błauż, A, Makal, A, Pawlędzio, S, Eurtivong, C, Arabshahi, HJ, Reynisson, J ORCID: https://orcid.org/0000-0003-4174-9512, Hartinger, CG, Rychlik, B and Plażuk, D (2021) Impact of the ferrocenyl group on cytotoxicity and KSP inhibitory activity of ferrocenyl monastrol conjugates. Dalton Transactions.

[img] Text
Manuscript_ACS_20210930 CH-JR.docx - Accepted Version
Restricted to Repository staff only until 12 November 2022.
Available under License Creative Commons Attribution Non-commercial.

Download (2MB)

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.

Item Type: Article
Additional Information: The final version of this article and all relevant information related to it, including copyrights and more, can be found on the publisher website at; https://pubs.rsc.org/en/content/articlelanding/2021/DT/D1DT03553C
Subjects: Q Science > QD Chemistry
Q Science > QD Chemistry > QD415 Biochemistry
R Medicine > R Medicine (General)
R Medicine > R Medicine (General) > R735 Medical education. Medical schools. Research
Divisions: Faculty of Medicine and Health Sciences > School of Pharmacy and Bioengineering
Related URLs:
Depositing User: Symplectic
Date Deposited: 26 Nov 2021 12:13
Last Modified: 26 Nov 2021 12:13
URI: https://eprints.keele.ac.uk/id/eprint/10310

Actions (login required)

View Item View Item