New melphalan derivatives for the treatment of retinoblastoma in combination with thermotherapy

Article Article scientifique Article New melphalan derivatives for the treatment of retinoblastoma in combination with thermotherapy eng 2024 author Zebret Soumaila Institute of Chemical Sciences and Engineering (ISIC), École Polytechnique Fédérale de Lausanne (EPFL) 1015 Lausanne Switzerland paul.dyson@epfl.ch. 525756 author Hadiji Mouna 0000-0001-8713-5597 Institute of Chemical Sciences and Engineering (ISIC), École Polytechnique Fédérale de Lausanne (EPFL) 1015 Lausanne Switzerland paul.dyson@epfl.ch. 834686 author Romano-deGea Jan 0000-0001-7340-4135 Institute of Chemical Sciences and Engineering (ISIC), École Polytechnique Fédérale de Lausanne (EPFL) 1015 Lausanne Switzerland paul.dyson@epfl.ch. author Bornet Aurélien Institute of Chemical Sciences and Engineering (ISIC), École Polytechnique Fédérale de Lausanne (EPFL) 1015 Lausanne Switzerland paul.dyson@epfl.ch. author Ortiz Daniel Institute of Chemical Sciences and Engineering (ISIC), École Polytechnique Fédérale de Lausanne (EPFL) 1015 Lausanne Switzerland paul.dyson@epfl.ch. author Fadaei-Tirani Farzaneh 0000-0002-7515-7593 Institute of Chemical Sciences and Engineering (ISIC), École Polytechnique Fédérale de Lausanne (EPFL) 1015 Lausanne Switzerland paul.dyson@epfl.ch. author Stathopoulos Christina Jules-Gonin Eye Hospital, Fondation Asile des Aveugles, University of Lausanne 1004 Lausanne Switzerland francis.munier@fa2.ch. 509628 author Nowak-Sliwinska Patrycja School of Pharmaceutical Sciences, University of Geneva 1211 Geneva Switzerland.,Institute of Pharmaceutical Sciences of Western Switzerland, University of Geneva 1211 Geneva Switzerland. 848409 Section des sciences pharmaceutiques (FARMA) author Munier Francis L Jules-Gonin Eye Hospital, Fondation Asile des Aveugles, University of Lausanne 1004 Lausanne Switzerland francis.munier@fa2.ch. author Dyson Paul J 0000-0003-3117-3249 Institute of Chemical Sciences and Engineering (ISIC), École Polytechnique Fédérale de Lausanne (EPFL) 1015 Lausanne Switzerland paul.dyson@epfl.ch. 2300-2304 10.1039/d4md00211c 39026655 2632-8682 PMC11253858 https://xlink.rsc.org/?DOI=D4MD00211C Of the different modalities used to treat retinoblastoma, a chemothermotherapeutic regimen combining carboplatin and thermotherapy (also termed focal therapy), and the application of melphalan as a monotherapy, are particularly successful. Some studies indicate that melphalan shows potential when applied in combination with focal therapy, and yet is not applied in this combination. Here we describe a series of synthetically modified melphalan derivatives that display enhanced cytotoxicity relative to melphalan itself, with some displaying further enhancements in cytotoxicity when applied in combination with heat (used as a model for thermotherapy). The synthetic approach, which involves modifying melphalan with perfluorous chains of varying lengths <i>via</i> an ester linker, could lead to a more effective treatment option for retinoblastoma with reduced side-effects, which is a key limitation of melphalan. Dewey 615 31 Section des sciences pharmaceutiques 17 false 1325 Pharmacologie moléculaire RSC medicinal chemistry 15 7 57762294-946d-4b39-b75d-b279939e1a14 Article (Published version) Public Article_scientifique_from_unpaywall.pdf 773266 application/pdf CC BY 17df91503bb0c9ee313a3a9987a4580e9a584951dfb2d2cb7d52c0389a2a5fa7 11cd5c67-4a3e-4dde-9d50-02113b04b0c4 Article (Published version) Public d4md00211c1.pdf 5639979 application/pdf a65385c4723f7bbb6f81ce9cd308c51415387ebc2324f17d48daa663f65c4cf4 openAccess Faculté des sciences / Section des sciences pharmaceutiques

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New melphalan derivatives for the treatment of retinoblastoma in combination with thermotherapy	RSC medicinal chemistry			2024	30	74

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