Metallodrugs against Breast Cancer: Combining the Tamoxifen Vector with Platinum(II) and Palladium(II) Complexes.

ABSTRACT: The luminal A-subtype of breast cancer, where the oestrogen receptor α (ERα) is overexpressed, is the most frequent one. The prodrug tamoxifen (1) is the clinically used agent, inhibiting the ERα activity via the formation of several active metabolites, such as 4-hydroxytamoxifen (2) or 4,4'-dihydroxytamoxifen (3). In this study, we present the tamoxifen derivative 4-[1,1-bis(4-methoxyphenyl)but-1-en-2-yl]-2,2'-bipyridine (4), which was combined with platinum or palladium dichloride, the former a well-known scaffold in anticancer treatment, to give [PtCl₂(4-κ²N,N')] (5) or [PdCl₂(4-κ²N,N'] (6). To prevent fast exchange of weakly coordinating chlorido ligands in aq

SUBMITTER: Kazimir A 

PROVIDER: S-EPMC9959148 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature