TY - JOUR
T1 - Cisplatin-eugenol Pt(IV) prodrugs target colon cancer stem cells
T2 - A novel strategy for enhanced anticancer efficacy
AU - Novohradsky, Vojtech
AU - Babu, Tomer
AU - Kostrhunova, Hana
AU - Plaskow, Menucha
AU - Markova, Lenka
AU - Acharya, Sourav
AU - Gibson, Dan
AU - Brabec, Viktor
N1 - Publisher Copyright:
© 2025
PY - 2025/2
Y1 - 2025/2
N2 - Platinum(IV) compounds possess distinct properties that set them apart from platinum(II) compounds. Often designed as prodrugs, they are reduced within cancer cells to their active platinum(II) form, enabling their cytotoxic effects. Their versatility also lies in their ability to be functionalized and conjugated with bioactive molecules to enhance cancer cell targeting. This report introduces new prodrugs that combine antitumor cisplatin with axially coordinated eugenol, leveraging their synergistic action to target cancer stem cells. A third bioactive ligand, 4-phenylbutyrate or octanoate, was added to further enhance biological activity, creating 'triple action' prodrugs. These new platinum(IV) prodrugs offer a novel approach to cancer therapy by improving targeting, increasing efficacy, overcoming drug resistance, and reducing tumor invasiveness while sparing healthy tissue.
AB - Platinum(IV) compounds possess distinct properties that set them apart from platinum(II) compounds. Often designed as prodrugs, they are reduced within cancer cells to their active platinum(II) form, enabling their cytotoxic effects. Their versatility also lies in their ability to be functionalized and conjugated with bioactive molecules to enhance cancer cell targeting. This report introduces new prodrugs that combine antitumor cisplatin with axially coordinated eugenol, leveraging their synergistic action to target cancer stem cells. A third bioactive ligand, 4-phenylbutyrate or octanoate, was added to further enhance biological activity, creating 'triple action' prodrugs. These new platinum(IV) prodrugs offer a novel approach to cancer therapy by improving targeting, increasing efficacy, overcoming drug resistance, and reducing tumor invasiveness while sparing healthy tissue.
KW - Cancer stem cells
KW - Cisplatin
KW - Eugenol
KW - Platinum(IV)
KW - Spheroids
UR - http://www.scopus.com/inward/record.url?scp=85215114661&partnerID=8YFLogxK
U2 - 10.1016/j.biopha.2025.117854
DO - 10.1016/j.biopha.2025.117854
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C2 - 39827811
AN - SCOPUS:85215114661
SN - 0753-3322
VL - 183
JO - Biomedicine and Pharmacotherapy
JF - Biomedicine and Pharmacotherapy
M1 - 117854
ER -