Synthesis and biological evaluation of novel daunorubicin-estrogen conjugates.

Steroids

PubMedID: 11522342

Kasiotis KM, Magiatis P, Pratsinis H, Skaltsounis A, Abadji V, Charalambous A, Moutsatsou P, Haroutounian SA. Synthesis and biological evaluation of novel daunorubicin-estrogen conjugates. Steroids. 2001;66(10):785-91.
The synthesis of two novel daunorubicin-estrogen conjugates with a steroidal and a non-steroidal ligand was undertaken in an attempt to target the cytotoxicity of anthracycline to estrogen-receptor positive cells. These conjugates (3 and 4), in contrast to their corresponding ligands, displayed weak binding affinities of 0.079 and 0.851 for the estrogen receptor. Conjugate 3 was consistently more cytotoxic than 4, which however showed some selectivity to estrogen receptor positive cell lines.