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Issue 5, 2015

In vivo evaluation of small-molecule thermoresponsive anticancer drugs potentiated by hyperthermia

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Abstract

Hyperthermia used as an adjuvant with chemotherapy is highly promising in the treatment of certain cancers. Currently, the small molecule drugs used in combination with hyperthermia were not designed for this application. Herein, we report the evaluation of a chlorambucil and a ruthenium compound modified with a long fluorous chain, which exhibit thermoresponsive activity in colorectal adenocarcinoma xenografts in athymic mice in combination with mild hyperthermia (42 °C). Intraperitoneal injection of the derivatives followed by local hyperthermia showed a synergistic tumor growth reduction by 79% and 90% for the chlorambucil and ruthenium-based derivatives, respectively, with the latter exhibiting a higher synergy in combination with hyperthermia compared to the monotherapies. Histological analysis shows that both derivatives in combination with hyperthermia significantly decrease the number of proliferating tumor cells.

Graphical abstract: In vivo evaluation of small-molecule thermoresponsive anticancer drugs potentiated by hyperthermia

Article information


Submitted
17 Feb 2015
Accepted
17 Mar 2015
First published
17 Mar 2015

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2015,6, 2795-2801
Article type
Edge Article
Author version available

In vivo evaluation of small-molecule thermoresponsive anticancer drugs potentiated by hyperthermia

C. M. Clavel, P. Nowak-Sliwinska, E. Păunescu, A. W. Griffioen and P. J. Dyson, Chem. Sci., 2015, 6, 2795 DOI: 10.1039/C5SC00613A

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