Search Results - "Lundeen, Scott G."
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The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening
Published in Bioorganic & medicinal chemistry letters (2007)“…A series of novel 2-(1H-indol-2-yl)-propan-2-ols have been designed, synthesized, and screened for their ability to inhibit testosterone-induced prostate…”
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2
Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands
Published in Bioorganic & medicinal chemistry letters (15-06-2006)“…A novel series of tetracyclic indoles ( I) have been designed, synthesized and evaluated as androgen receptor (AR) ligands. Studies of structure–activity…”
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3
Characterization of the Ovariectomized Rat Model for the Evaluation of Estrogen Effects on Plasma Cholesterol Levels
Published in Endocrinology (Philadelphia) (01-04-1997)“…Estrogens protect against cardiovascular disease in women through effects on the vascular wall and liver. Here we further characterize the rat as a model for…”
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4
Synthesis and SAR of tetracyclic pyrroloquinolones as phosphodiesterase 5 inhibitors
Published in Bioorganic & medicinal chemistry (15-03-2004)“…The synthesis of the fused tetracyclic pyrroloquinolones 9a– i in four steps is described. The PDE5 inhibitory activities of these compounds, their…”
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5
Design, Synthesis, and in Vivo SAR of a Novel Series of Pyrazolines as Potent Selective Androgen Receptor Modulators
Published in Journal of medicinal chemistry (09-08-2007)“…A novel series of pyrazolines 2 have been designed, synthesized, and evaluated by in vivo screening as tissue-selective androgen receptor modulators (SARMs)…”
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6
Pharmacological characterization of an imidazolopyrazole as novel selective androgen receptor modulator
Published in The Journal of steroid biochemistry and molecular biology (01-03-2013)“…► SARMs have anabolic activity on muscle over prostate. ► The imidazolopyrazole was discovered as SARM agonist with mixed agonistic and antagonistic activities…”
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7
Discovery and structure-activity relationships of a novel series of benzopyran-based K(ATP) openers for urge urinary incontinence
Published in Bioorganic & medicinal chemistry (15-01-2009)“…A novel series of benzopyran derivatives were synthesized and evaluated as K(ATP) channel openers. Structure-activity relationships were investigated around…”
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8
Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators
Published in Bioorganic & medicinal chemistry letters (15-11-2006)“…A novel series of hydantoin derivatives were identified by in vivo studies as tissue selective androgen receptor modulators. SAR around this series revealed…”
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Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold
Published in Bioorganic & medicinal chemistry letters (15-03-2007)“…The synthesis and in vivo SAR of 2-(2,2,2)-trifluoroethyl-benzimidazoles are described. Prostate antagonism and/or levator ani agonism can be modulated by…”
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10
Emerging role of genomics in endometriosis research
Published in Fertility and sterility (01-10-2002)“…Rapidly evolving methods in genomics and proteomics research already are changing the nature of biomedical investigation. In this report we briefly review some…”
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11
Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators
Published in Bioorganic & medicinal chemistry letters (15-01-2007)“…A novel imidazolopyrazole derivative has been fortuitously discovered as potent selective androgen receptor modulator with in vivo efficacy. A novel…”
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12
Discovery and structure-activity relationships of a novel series of benzopyran-based KATP openers for urge urinary incontinence
Published in Bioorganic & medicinal chemistry (15-01-2009)“…A novel series of benzopyran derivatives were synthesized and evaluated as KATP channel openers. Structure-activity relationships were investigated around…”
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13
A selective androgen receptor modulator with minimal prostate hypertrophic activity enhances lean body mass in male rats and stimulates sexual behavior in female rats
Published in Endocrine (01-08-2007)“…Androgen receptor (AR) ligands with tissue selectivity (selective androgen receptor modulators, or SARMs) have potential for treating muscle wasting,…”
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14
Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives
Published in Bioorganic & medicinal chemistry letters (01-02-2007)“…The synthesis and in vivo SAR of 5,6-dichloro-benzimidazole derivatives as novel selective androgen receptor antagonists are described. During screening of…”
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15
2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-02-2007)“…The synthesis and in vivo SAR of N-benzyl, N-aceto, and N-ethylene ether derivatives of 2-(2,2,2-trifluoroethyl)-5,6-dichloro-benzimidazole as novel androgen…”
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16
Synthesis and identification of novel 11β-aryl-4′,5′-dihydrospiro[estra-4,9-diene-17β,4′-oxazole] analogs with dissociated antiprogesterone activities
Published in Bioorganic & medicinal chemistry letters (01-11-2007)“…A series of novel 11β-aryl-4′,5′-dihydrospiro[estra-4,9-diene-17β,4′-oxazole] analogs have been synthesized and evaluated for their antiprogesterone and…”
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17
Cell type-specific bidirectional regulation of the glucocorticoid-induced leucine zipper (GILZ) gene by estrogen
Published in The Journal of steroid biochemistry and molecular biology (01-08-2004)“…Estrogen has numerous beneficial physiological actions; however, by acting as a mitogen, it plays a significant role in the induction and maintenance of breast…”
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Rat uterine complement C3 expression as a model for progesterone receptor modulators: characterization of the new progestin trimegestone
Published in The Journal of steroid biochemistry and molecular biology (01-08-2001)“…Progestins have a wide variety of activities in female reproduction. There are also pharmacological applications for progestins, including hormone replacement…”
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19
Altered activities of cyclic nucleotide phosphodiesterases and soluble guanylyl cyclase in cultured RFL-6 cells
Published in The international journal of biochemistry & cell biology (01-10-2004)“…We utilized rat fetal lung fibroblasts (RFL-6) to evaluate our PDE5 inhibitors at cellular level and observed a decrease in cGMP accumulation induced by sodium…”
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In vitro characterization of trimegestone: a new potent and selective progestin
Published in Steroids (01-10-2000)“…Trimegestone (TMG) is a novel 19-norpregnane progestin under development for hormone replacement therapy and oral contraception. The objective of the current…”
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