Synthesis and biological evaluation of novel daunorubicin-estrogen conjugates |
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| Authors: | Kasiotis K M Magiatis P Pratsinis H Skaltsounis A Abadji V Charalambous A Moutsatsou P Haroutounian S A |
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| Affiliation: | Chemistry Lab., Agric. University of Athens, Iera odos 75, 11855, Athens, Greece. |
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| Abstract: | 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. |
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