Journal of medicinal chemistry, 2007-09, Vol.50 (19), p.4699-4709
2007
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and Characterization of Nonsteroidal Glucocorticoid Receptor Modulators for Multiple Myeloma
- Ist Teil von
- Journal of medicinal chemistry, 2007-09, Vol.50 (19), p.4699-4709
- Ort / Verlag
- Washington, DC: American Chemical Society
- Erscheinungsjahr
- 2007
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm070370zTitel-ID: cdi_proquest_miscellaneous_68274658
- Format
- –
- Schlagworte
- Animals, Antineoplastic agents, Antineoplastic Agents - chemical synthesis, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacology, Benzopyrans - chemical synthesis, Benzopyrans - chemistry, Benzopyrans - pharmacology, Binding, Competitive, Biological and medical sciences, Dexamethasone - pharmacology, General aspects, Humans, Medical sciences, Mice, Mineralocorticoid Receptor Antagonists, Models, Molecular, Multiple Myeloma - drug therapy, Multiple Myeloma - pathology, Pharmacology. Drug treatments, Quinolines - chemical synthesis, Quinolines - chemistry, Quinolines - pharmacology, Receptors, Glucocorticoid - agonists, Receptors, Glucocorticoid - antagonists & inhibitors, Receptors, Glucocorticoid - drug effects, Receptors, Mineralocorticoid - agonists, Stereoisomerism, Structure-Activity Relationship, Xenograft Model Antitumor Assays