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


ABSTRACT: 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 via an ester linker, could lead to a more effective treatment option for retinoblastoma with reduced side-effects, which is a key limitation of melphalan.

SUBMITTER: Zebret S 

PROVIDER: S-EPMC11253858 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature

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

Zebret Soumaila S   Hadiji Mouna M   Romano-deGea Jan J   Bornet Aurélien A   Ortiz Daniel D   Fadaei-Tirani Farzaneh F   Stathopoulos Christina C   Nowak-Sliwinska Patrycja P   Munier Francis L FL   Dyson Paul J PJ  

RSC medicinal chemistry 20240521 7


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 relati  ...[more]

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