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Thermoresponsive carboplatin-releasing prodrugs.
McAdam, Aemilia D; Batchelor, Lucinda K; Romano-deGea, Jan; Vasilyev, Dmitry; Dyson, Paul J.
Affiliation
  • McAdam AD; Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
  • Batchelor LK; Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
  • Romano-deGea J; Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
  • Vasilyev D; Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
  • Dyson PJ; Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland. Electronic address: paul.dyson@epfl.ch.
J Inorg Biochem ; 254: 112505, 2024 05.
Article in En | MEDLINE | ID: mdl-38377623
ABSTRACT
Platinum-based anticancer drugs, while potent, are associated with numerous and severe side effects. Hyperthermia therapy is an effective adjuvant in anticancer treatment, however, clinically used platinum drugs have not been optimised for combination with hyperthermia. The derivatisation of existing anticancer drugs with appropriately chosen thermoresponsive moieties results in drugs being activated only at the heated site. Perfluorinated chains of varying lengths were installed on carboplatin, a clinically approved drug, leading to the successful synthesis of a series of mono- and di- substituted platinum(IV) carboplatin prodrugs. Some of these complexes display relevant thermosensitivity on ovarian cancer cell lines, i.e., being inactive at 37 °C while having comparable activity to carboplatin under mild hyperthermia (42 °C). Nuclear magnetic resonance spectroscopy and mass spectrometry indicated that carboplatin is likely the active platinum(II) anticancer agent upon reduction and cyclic voltammetry revealed that the length of the fluorinated alkyl chain has a strong influence on the rate of carboplatin formation, regulating the subsequent cytotoxicity.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Ovarian Neoplasms / Prodrugs / Antineoplastic Agents Limits: Female / Humans Language: En Journal: J Inorg Biochem Year: 2024 Document type: Article Affiliation country: Switzerland Country of publication: United States

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Ovarian Neoplasms / Prodrugs / Antineoplastic Agents Limits: Female / Humans Language: En Journal: J Inorg Biochem Year: 2024 Document type: Article Affiliation country: Switzerland Country of publication: United States