1.
Chem Biodivers
; 20(1): e202201025, 2023 Jan.
Artigo
em Inglês
| MEDLINE
| ID: mdl-36427041
RESUMO
Phthalidyl promoiety has been used in several drugs, but they were all marketed in racemic form. The pharmaceutical effects of each enantiomer have not been clearly demonstrated. In this project, an anticancer chemotherapy drug, chlorambucil, was modified as enantiopure phthalidyl prodrugs. The enantiomers, together with phthalidyl unit and their racemic mixture, were then subject to the inâ vivo bioactivity tests against B16F10 melanoma cells. It was found that proper chirality within the promoiety had noticeably better inâ vivo pharmacological effects than the parent drug, the enantiomer and racemic mixture. This merit perhaps could be extended from the phthalidyl prodrugs to other chirality containing prodrugs.