title: 1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
abstract: 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.
authors.affiliation: Chemical Sciences, Pfizer Global Research and Development, 500 Arcola Road, Collegeville, PA 19426, USA. Jkern75@hotmail.com
authors.forename: Jeffrey C
authors.initials: JC
authors.lastname: Kern
authors.forename: Eugene
authors.initials: E
authors.lastname: Terefenko
authors.forename: Eugene
authors.initials: E
authors.lastname: Trybulski
authors.forename: Thomas J
authors.initials: TJ
authors.lastname: Berrodin
authors.forename: Jeffrey
authors.initials: J
authors.lastname: Cohen
authors.forename: Richard C
authors.initials: RC
authors.lastname: Winneker
authors.forename: Matthew R
authors.initials: MR
authors.lastname: Yudt
authors.forename: Zhiming
authors.initials: Z
authors.lastname: Zhang
authors.forename: Yuan
authors.initials: Y
authors.lastname: Zhu
authors.forename: Puwen
authors.initials: P
authors.lastname: Zhang
mesh_terms: D000469:Alkaline Phosphatase / Q000378:metabolism; D045744:Cell Line, Tumor; D006801:Humans; D011758:Pyrroles / Q000737:chemistry*; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D011758:Pyrroles; D011980:Receptors, Progesterone; D013764:Tetrahydronaphthalenes; D000469:Alkaline Phosphatase