β-Lactam Estrogen Receptor Antagonists and a Dual-Targeting Estrogen Receptor/Tubulin Ligand
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چکیده
منابع مشابه
β-Lactam estrogen receptor antagonists and a dual-targeting estrogen receptor/tubulin ligand.
Twelve novel β-lactams were synthesized and their antiproliferative effects and binding affinity for the predominant isoforms of the estrogen receptor (ER), ERα and ERβ, were determined. β-Lactams 23 and 26 had the strongest binding affinities for ERα (IC50 values: 40 and 8 nM, respectively) and ERβ (IC50 values: 19 and 15 nM). β-Lactam 26 was the most potent in antiproliferative assays using M...
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The existence of two rather than one estrogen receptor, today characterized as estrogen receptor a (ERa) and estrogen receptor b (ERb), indicates that the mechanism of action of 17b-estradiol and related synthetic drugs is more complex than previously thought. Because the homology of amino acid residues in the ligand-binding domain (LBD) of ERb is high compared with those amino acid residues in...
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To develop compounds that are antagonists on ER , but not ER , we have added basic side-chains typically found in nonsteroidal antiestrogens to pyrazole compounds that bind with much higher affinity to ER than to ER . In this way we have developed basic side-chain pyrazoles (BSC-pyrazoles) that are high affinity, potent, selective antagonists on ER . These BSCpyrazoles are themselves inactive o...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2014
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm500670d