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Your search keyword '"William W. Lamph"' showing total 3 results
Start Over Author "William W. Lamph" Journal journal of medicinal chemistry
3 results on '"William W. Lamph"'

1. Synthesis and Characterization of Nonsteroidal Glucocorticoid Receptor Modulators for Multiple Myeloma

Author

Jeffrey N. Miner, Deepa Rungta, Lino J. Valdez, Yongkai Li, Andrew Hudson, William W. Lamph, Jean Yen, Dean P. Phillips, and Andrés Negro-Vilar, Lin Zhi, Angie Vassar, Catalina Cuervo, Reid P. Bissonnette, Keith B. Marschke, E. Adam Kallel, Mark E. Adams, Catherine J. Gharbaoui, Robert I. Higuchi, Dale E. Mais, and Steven L. Roach

Subjects
Models, Molecular, medicine.medical_specialty, Antineoplastic Agents, Pharmacology, Binding, Competitive, Dexamethasone, Mice, Structure-Activity Relationship, Receptors, Glucocorticoid, Mineralocorticoid receptor, Glucocorticoid receptor, In vivo, Internal medicine, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Benzopyrans, Receptor, Cytotoxicity, Mineralocorticoid Receptor Antagonists, Chemistry, Stereoisomerism, Xenograft Model Antitumor Assays, In vitro, Receptors, Mineralocorticoid, Endocrinology, Quinolines, Molecular Medicine, Multiple Myeloma, medicine.drug
Abstract

Structure-activity relationship studies centered around 3'-substituted (Z)-5-(2'-(thienylmethylidene))1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-chromeno[3,4-f]quinolines are described. A series of highly potent and efficacious selective glucocorticoid receptor modulators were identified with in vitro activity comparable to dexamethasone. In vivo evaluation of these compounds utilizing a 28 day mouse tumor xenograft model demonstrated efficacy equal to dexamethasone in the reduction of tumor volume.

Published
2007
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2. Discovery of Novel Retinoic Acid Receptor Agonists Having Potent Antiproliferative Activity in Cervical Cancer Cells

Author

William W. Lamph, Alex M. Nadzan, Richard A. Heyman, Deborah L. Love, Dale E. Mais, Lin Zhang, Glenn Croston, and Marcus F. Boehm

Subjects
Receptors, Retinoic Acid, medicine.drug_class, Retinoic acid, Uterine Cervical Neoplasms, Antineoplastic Agents, Retinoid X receptor, Retinoids, chemistry.chemical_compound, Drug Discovery, Tumor Cells, Cultured, medicine, Humans, Retinoid, Molecular Structure, Retinoid X receptor alpha, Chemistry, Retinoid X receptor gamma, Retinoic acid receptor, Retinoid X Receptors, Biochemistry, Retinoic acid receptor alpha, Cancer research, Molecular Medicine, Female, Drug Screening Assays, Antitumor, Retinoid X receptor beta, Cell Division, Thymidine, Transcription Factors
Abstract

Retinoic acid receptor (RAR) active retinoids have proven therapeutically useful for treating certain cancers and dermatological diseases. Herein, we describe the discovery of two new RAR active trienoic acid retinoids, (2E,4E,6E)-7-(3,5-di-tert-butylphenyl)-3-methylocta-2, 4,6-trienoic acid (10a, ALRT1550) and (2E,4E,6Z)-7-(3,5-di-tert-butylphenyl)-3-methylocta-2, 4,6-trienoic acid (10b, LG100567). ALRT1550 is a RAR selective retinoid which exhibits exceptional potency in both competitive binding and cotransfection assays. Moreover, it is the most potent antiproliferative retinoid described to date and thus has implications for the treatment of certain cancers. LG100567 is a potent panagonist which activates both RARs and retinoid X receptors.

Published
1996
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