Synthesis and biological activities of nucleoside-estradiol conjugates.
Nucleosides were coupled to estradiol via a 17alpha-ethynyl spacer group using Pd(II) as a catalyst. The conjugates were evaluated in vitro for estrogen receptor (ER) binding affinity and cytotoxicity against cell lines with and without ER. The highest receptor binding affinities (RBA approximately 3) were observed with conjugates coupled via a relative long spacer group, while none of the conjugates exhibited cytotoxicity against either cell lines.
Ali
Hasrat
H
Department of Nuclear Medicine and Radiobiology, Faculty of Medicine, Université de Sherbrooke, Sherbrooke, Quebec, Canada J1H 5N4.
Ahmed
Naseem
N
Tessier
Guillaume
G
van Lier
Johan E
JE
D001665:Binding Sites; D002384:Catalysis; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D004958:Estradiol / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D015394:Molecular Structure; D009705:Nucleosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010165:Palladium / Q000737:chemistry; D011960:Receptors, Estrogen / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
D009705:Nucleosides; D011960:Receptors, Estrogen; D004958:Estradiol; D010165:Palladium