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Your search keyword '"Thomas J, Berrodin"' showing total 2 results
Start Over Author "Thomas J, Berrodin" Journal bioorganicmedicinal chemistry letters
2 results on '"Thomas J, Berrodin"'

1. 5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators

Author

Matthew R. Yudt, Richard C. Winneker, Yuan Zhu, Puwen Zhang, Jeffrey I. Cohen, Terefenko Eugene Anthony, Eugene John Trybulski, Zhiming Zhang, Jeffrey Curtis Kern, and Thomas J. Berrodin

Subjects
Agonist, medicine.drug_class, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Structure-Activity Relationship, Drug Discovery, Progesterone receptor, medicine, Molecular Biology, Molecular Structure, Organic Chemistry, Antagonist, Biological activity, Stereoisomerism, Oxime, chemistry, Nuclear receptor, Drug Design, Indans, Molecular Medicine, Alkaline phosphatase, Receptors, Progesterone
Abstract

Novel 5-aryl indanones, inden-1-one oximes, and inden-1-ols were synthesized and evaluated as progesterone receptor (PR) modulators using the T47D cell alkaline phosphatase assay. Both PR agonists and antagonists were achieved with appropriate 3- and 5-substitution from indanones and inden-1-ols while inden-1-one oximes provided only PR antagonists. Several compounds such as 10 and 11 demonstrated potent in vitro PR agonist potency similar to that of steroidal progesterone (1). In addition, a number of compounds (e.g., 12, 13, 17, 18) showed potent PR antagonist activity indicating the indanones and derivatives are promising PR modulator templates.

Published
2009

2. 1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators

Author

Puwen Zhang, Matthew R. Yudt, Zhiming Zhang, Andrew Fensome, Jay E. Wrobel, Jeffrey Curtis Kern, Richard C. Winneker, Ray Unwalla, Yuan Zhu, Terefenko Eugene Anthony, Jeffrey I. Cohen, and Thomas J. Berrodin

Subjects
Agonist, Stereochemistry, medicine.drug_class, medicine.medical_treatment, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Chemical synthesis, Steroid, Structure-Activity Relationship, Drug Discovery, Progesterone receptor, medicine, Combinatorial Chemistry Techniques, Humans, Receptor, Molecular Biology, Bicyclic molecule, Molecular Structure, Chemistry, Organic Chemistry, Antagonist, Oxazepines, Molecular Medicine, Alkaline phosphatase, Receptors, Progesterone
Abstract

A series of novel 7-(5'-cyanopyrrol-2-yl) substituted benzo[1,4]oxazepin-2-ones were prepared and tested for their progesterone receptor (PR) agonist or antagonist activity in the alkaline phosphatase assay using the human T47D breast carcinoma cell line. Both PR agonists and antagonists were achieved with an appropriate choice of 5-substitution. Several analogs were potent PR agonists (e.g., 12 and 13) or PR antagonists (e.g., 18) with good selectivity over other steroid receptors.

Published
2008

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