期刊
DALTON TRANSACTIONS
卷 51, 期 2, 页码 491-508出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1dt03553c
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资金
- National Science Centre Poland (NCN) [UMO-2015/17/B/ST5/02331]
Incorporating the ferrocenyl moiety into a bioactive molecule can significantly alter the activity of the resulting conjugate. By applying this strategy, ferrocenyl analogs of monastrol were designed with higher antiproliferative activity and KSP modulatory activity, attributed to the presence of the ferrocenyl group.
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.
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