Synthesis and biological evaluation of novel daunorubicin-estrogen conjugates.
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.
Kasiotis
K M
KM
Chemistry Lab., Agric. University of Athens, Iera odos 75, 11855, Athens, Greece.
Magiatis
P
P
Pratsinis
H
H
Skaltsounis
A
A
Abadji
V
V
Charalambous
A
A
Moutsatsou
P
P
Haroutounian
S A
SA
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis; D002460:Cell Line; D003630:Daunorubicin / Q000737:chemistry* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004967:Estrogens / Q000737:chemistry* / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008024:Ligands; D008297:Male; D051379:Mice; D008875:Middle Aged; D015394:Molecular Structure; D011960:Receptors, Estrogen / Q000378:metabolism
D000970:Antineoplastic Agents; D004967:Estrogens; D008024:Ligands; D011960:Receptors, Estrogen; D003630:Daunorubicin