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Your search keyword '"Gayo Leah M"' showing total 7 results
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7 results on '"Gayo Leah M"'

1. Synthetic utility of alkenylcyclobutenedione monoketals: Michael additions and the synthesis of a natural benzofuranosesquiterpenequinone

Author

Liu, Hui, Gayo, Leah M., Sullivan, Robert W., Choi, Angela Y.H., and Moore, Harold W.

Subjects
Quinone -- Research, Chemical reactions -- Analysis, Biological sciences, Chemistry
Abstract

A method for the synthesis of highly substituted cyclobutenone, which allows the modifications of alkenyl substituents through 1,6-addition reactions of different nucleophiles, is described. This technique is extended for the synthesis of quinones having unsaturated group at the 4-position. The efficiency of this technique is proved by the regiospecific synthesis of a series of benzofuranosesquiterpenequinones.

Published
1994

2. A potentially general regiospecific synthesis of substituted quinones from dimethyl squarate

Author

Gayo, Leah M., Winters, Michael P., and Moore, Harold W.

Subjects
Quinone -- Research, Organometallic compounds -- Research, Cyclic compounds -- Research, Biological sciences, Chemistry
Abstract

A method for the regiospecific synthesis of benzoquinones and naphthaquinones was reported. The preparation starts with dimethyl squarate which upon addition of an organolithium reagent gives cyclobutenone. Methanolysis then follows to give cyclobutenedione monoketals. Treatment with a second organolithium reagent and trifluoroacetic anhydride gives other monoketals which upon hydrolysis lead to the synthetic intermediates.

Published
1992

3. Lead identification of a potent benzopyranone selective estrogen receptor modulator

Author

Adam Kois, Normand Richard, Khammungkhune Sak, Graziella I. Shevlin, Shripad S. Bhagwat, John Sapienza, Helen Brady, Mathew Hickman, Jalluri Ravi Kumar, Deborah Mortensen, Gayo Leah M, Jeffrey A. Mckie, Mary Doubleday, May S Kung Sutherland, and Bernd Stein

Subjects
Clinical Biochemistry, Cell, Pharmaceutical Science, Pharmacology, Biochemistry, chemistry.chemical_compound, Estrogen Receptor Modulators, Piperidines, Coumarins, Drug Discovery, medicine, Tumor Cells, Cultured, Animals, Raloxifene, Molecular Biology, Binding Sites, Estradiol, Molecular Structure, Chemistry, Interleukin-6, Organic Chemistry, Estrogen Antagonists, Estrogen Receptor alpha, Ligand (biochemistry), In vitro, Tamoxifen, medicine.anatomical_structure, Selective estrogen receptor modulator, Raloxifene Hydrochloride, Molecular Medicine, Female, Estrogen receptor alpha, Lead compound, hormones, hormone substitutes, and hormone antagonists, medicine.drug
Abstract

Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release.

Published
2002

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