1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists

Non-steroidal 1-methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalenes and acyclic derivatives were evaluated as novel series of progesterone receptor (PR) antagonists using the T47D cell alkaline phosphatase assay. Moderate to potent PR antagonists were achieved with these scaffolds. Se...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-08, Vol.20 (16), p.4816-4818
Hauptverfasser:	KERN, Jeffrey C, TEREFENKO, Eugene, TRYBULSKI, Eugene, BERRODIN, Thomas J, COHEN, Jeffrey, WINNEKER, Richard C, YUDT, Matthew R, ZHIMING ZHANG, YUAN ZHU, PUWEN ZHANG
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkaline Phosphatase - metabolism Biological and medical sciences Cell Line, Tumor Hormones. Endocrine system Humans Medical sciences Pharmacology. Drug treatments Pyrroles - chemistry Receptors, Progesterone - antagonists & inhibitors Receptors, Progesterone - metabolism Structure-Activity Relationship Tetrahydronaphthalenes - chemical synthesis Tetrahydronaphthalenes - chemistry Tetrahydronaphthalenes - pharmacology
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Zusammenfassung:	Non-steroidal 1-methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalenes and acyclic derivatives were evaluated as novel series of progesterone receptor (PR) antagonists using the T47D cell alkaline phosphatase assay. Moderate to potent PR antagonists were achieved with these scaffolds. Several compounds (e.g., 15 and 20) demonstrated low nanomolar PR antagonist potency and good selectivity versus other steroid receptors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.06.109