Author: "Hayes EC" / Topic: receptors, estrogen - Searchworks@Jio Institute Digital Library Search Results

Author: Blizzard TA, DiNinno F, Chen HY, Kim S, Wu JY, Chan W, Birzin ET, Yang YT, Pai LY, Hayes EC, DaSilva CA, Rohrer SP, Schaeffer JM, and Hammond ML
Subjects: Animals, Breast Neoplasms drug therapy, Breast Neoplasms pathology, Cell Line, Tumor, Dose-Response Relationship, Drug, Estrogen Antagonists chemical synthesis, Estrogen Antagonists pharmacology, Female, Humans, Oxathiins pharmacology, Rats, Receptors, Estrogen metabolism, Selective Estrogen Receptor Modulators pharmacology, Structure-Activity Relationship, Uterus drug effects, Uterus growth & development, Oxathiins chemical synthesis, Receptors, Estrogen chemistry, Selective Estrogen Receptor Modulators chemical synthesis
Abstract: An optimized side chain for dihydrobenzoxathiin SERAMs was discovered and attached to four dihydrobenzoxathiin platforms. The novel SERAMs show exceptional estrogen antagonist activity in uterine tissue and an MCF-7 breast cancer cell assay.
Published: 2005
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Author: Blizzard TA, Dininno F, Morgan JD 2nd, Chen HY, Wu JY, Kim S, Chan W, Birzin ET, Yang YT, Pai LY, Fitzgerald PM, Sharma N, Li Y, Zhang Z, Hayes EC, Dasilva CA, Tang W, Rohrer SP, Schaeffer JM, and Hammond ML
Subjects: Ligands, Models, Molecular, Oxathiins chemistry, Receptors, Estrogen metabolism, Oxathiins pharmacology, Pyrrolidines chemistry, Receptors, Estrogen drug effects, Selective Estrogen Receptor Modulators pharmacology
Abstract: A series of dihydrobenzoxathiin SERAMs with alkylated pyrrolidine side chains or alkylated linkers was prepared. Minor modifications in the side chain or linker resulted in significant effects on biological activity, especially in uterine tissue.
Published: 2005
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Author: Blizzard TA, DiNinno F, Morgan JD 2nd, Chen HY, Wu JY, Gude C, Kim S, Chan W, Birzin ET, Tien Yang Y, Pai LY, Zhang Z, Hayes EC, DaSilva CA, Tang W, Rohrer SP, Schaeffer JM, and Hammond ML
Subjects: Animals, Bridged Bicyclo Compounds pharmacology, Female, Kinetics, Models, Molecular, Molecular Conformation, Selective Estrogen Receptor Modulators chemistry, Selective Estrogen Receptor Modulators pharmacology, Structure-Activity Relationship, Uterus drug effects, Bridged Bicyclo Compounds chemistry, Ligands, Receptors, Estrogen metabolism, Selective Estrogen Receptor Modulators metabolism
Abstract: A series of benzoxathiin SERAMs with bicyclic amine side chains was prepared. Minor modifications in the side chain resulted in significant effects on biological activity, especially in uterine tissue.
Published: 2004
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Author: Blizzard TA, DiNinno F, Morgan JD 2nd, Wu JY, Chen HY, Kim S, Chan W, Birzin ET, Yang YT, Pai LY, Zhang Z, Hayes EC, DaSilva CA, Tang W, Rohrer SP, Schaeffer JM, and Hammond ML
Subjects: Animals, Female, Kinetics, Ligands, Models, Molecular, Molecular Conformation, Selective Estrogen Receptor Modulators chemistry, Selective Estrogen Receptor Modulators pharmacology, Structure-Activity Relationship, Uterus drug effects, Receptors, Estrogen metabolism, Selective Estrogen Receptor Modulators metabolism
Abstract: A series of benzoxathiin SERAMs with heteroatom-substituted amine side chains was prepared. Minor modifications in the side chain resulted in significant effects on biological activity, especially in uterine tissue.
Published: 2004
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Author: Tan Q, Birzin ET, Chan W, Tien Yang Y, Pai LY, Hayes EC, DaSilva CA, DiNinno F, Rohrer SP, Schaeffer JM, and Hammond ML
Subjects: Binding Sites, Cell Line, Tumor, Estrogen Antagonists pharmacology, Estrogen Receptor alpha antagonists & inhibitors, Estrogen Receptor beta antagonists & inhibitors, Humans, Ligands, Oxathiins pharmacology, Structure-Activity Relationship, Estrogen Antagonists chemical synthesis, Oxathiins chemical synthesis, Receptors, Estrogen metabolism
Abstract: Dihydrobenzoxathiin analogs (1-11) with modifications on the basic side chain region were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The compounds generally maintained a high degree of selectivity for ERalpha over ERbeta, similar to the original lead compound I. Many of the compounds also maintained high potency in the inhibition of human carcinoma MCF-7 cell growth. However, all were less potent in the inhibition of estradiol-triggered uterine growth. This work demonstrates the sensitive nature of modification to the antagonist basic side chain region.
Published: 2004
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Author: Tan Q, Birzin ET, Chan W, Yang YT, Pai LY, Hayes EC, DaSilva CA, DiNinno F, Rohrer SP, Schaeffer JM, and Hammond ML
Subjects: Animals, Binding Sites, Cells, Cultured, Estrogen Receptor alpha, Estrogen Receptor beta, Female, Heterocyclic Compounds, 2-Ring pharmacology, Inhibitory Concentration 50, Ligands, Models, Biological, Piperidines pharmacology, Rats, Selective Estrogen Receptor Modulators pharmacology, Structure-Activity Relationship, Uterus drug effects, Uterus metabolism, Heterocyclic Compounds, 2-Ring chemical synthesis, Piperidines chemical synthesis, Receptors, Estrogen metabolism, Selective Estrogen Receptor Modulators chemical synthesis
Abstract: Dihydrobenzodithiin compounds (1-6) were prepared to explore the expansion of the dihydrobenzoxathiin lead compounds I-III as SERAMs (Selective Estrogen Receptor Alpha Modulators). The dihydrobenzodithiin compounds generally maintained a high degree of selectivity for ERalpha over ERbeta, however, they lacked the in vivo antagonism/agonism activity exhibited by the lead class in an immature rat uterine growth model.
Published: 2004
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