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ROS‐Responsive N‐Alkylaminoferrocenes for Cancer‐Cell‐Specific Targeting of Mitochondria.

Authors :
Reshetnikov, Viktor
Daum, Steffen
Janko, Christina
Karawacka, Weronika
Tietze, Rainer
Alexiou, Christoph
Paryzhak, Solomiya
Dumych, Tetiana
Bilyy, Rostyslav
Tripal, Philipp
Schmid, Benjamin
Palmisano, Ralf
Mokhir, Andriy
Source :
Angewandte Chemie; 9/10/2018, Vol. 130 Issue 37, p12119-12122, 4p
Publication Year :
2018

Abstract

Abstract: Mitochondrial membrane potential is more negative in cancer cells than in normal cells, allowing cancer targeting by delocalized lipophilic cations (DLCs). However, as the difference is rather small, these drugs affect also normal cells. Now a concept of pro‐DLCs is proposed based on an N‐alkylaminoferrocene structure. These prodrugs are activated by the reaction with reactive oxygen species (ROS) forming ferrocenium‐based DLCs. Since ROS are overproduced in cancer, the high‐efficiency cancer‐cell‐specific targeting of mitochondria could be achieved as demonstrated by fluorescence microscopy in combination with two fluorogenic pro‐DLCs in vitro and in vivo. We prepared a conjugate of another pro‐DLC with a clinically approved drug carboplatin and confirmed that its accumulation in mitochondria was higher than that of the free drug. This was reflected in the substantially higher anticancer effect of the conjugate. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
00448249
Volume :
130
Issue :
37
Database :
Complementary Index
Journal :
Angewandte Chemie
Publication Type :
Academic Journal
Accession number :
131621475
Full Text :
https://doi.org/10.1002/ange.201805955