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Your search keyword '"Marquis L. Cummings"' showing total 2 results
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2 results on '"Marquis L. Cummings"'

1. Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity

Author

Esther Martinborough, Donald S. Karanewsky, Francisco J. López, Robert I. Higuchi, Min Wu, William Y. Chang, Marquis L. Cummings, Lin Zhi, Thomas Lau, Yun Oliver Long, Thomas R. Caferro, and Keith B. Marschke

Subjects
Male, medicine.medical_specialty, medicine.drug_class, Clinical Biochemistry, Administration, Oral, Pharmaceutical Science, Quinolones, Biochemistry, Rats, Sprague-Dawley, Structure-Activity Relationship, Anabolic Agents, In vivo, Internal medicine, Oxazines, Drug Discovery, Androgen Receptor Antagonists, medicine, Animals, Structure–activity relationship, Testosterone, Receptor, Molecular Biology, Chemistry, Organic Chemistry, Prostate, Organ Size, Androgen, Rats, Androgen receptor, Endocrinology, Models, Chemical, Selective androgen receptor modulator, Receptors, Androgen, Androgens, Molecular Medicine, Orchiectomy
Abstract

Modification on a lead series of [1,4]oxazino[3,2-g]quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintenance of levator ani muscle at 3mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay.

Published
2008

2. Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones

Author

Jyun-Hung Chen, Thomas R. Caferro, Charlotte Pooley Deckhut, Lin Zhi, Christopher M. Tegley, Keith B. Marschke, Anthony W. Thompson, James P. Edwards, E. Adam Kallel, Marquis L. Cummings, Francisco J. López, William T. Schrader, Robert I. Higuchi, Mark E. Adams, and Donald S. Karanewsky

Subjects
Male, Models, Molecular, medicine.medical_specialty, medicine.drug_class, Clinical Biochemistry, Pharmaceutical Science, Quinolones, Biochemistry, Article, Cell Line, Structure-Activity Relationship, In vivo, Internal medicine, Oxazines, Drug Discovery, medicine, Animals, Humans, Potency, Structure–activity relationship, Testosterone, Receptor, Molecular Biology, Dose-Response Relationship, Drug, Chemistry, Organic Chemistry, Receptors, Somatotropin, Androgen, Rats, Androgen receptor, Endocrinology, Selective androgen receptor modulator, Receptors, Androgen, Molecular Medicine, Indicators and Reagents, Receptors, Progesterone, Orchiectomy
Abstract

A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar potency in vitro. Compound 18h demonstrated full efficacy in the maintenance of muscle weight, at 10 mg/kg, with reduced activity in prostate weight in an in vivo model of androgen action.

Published
2007

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