Novel estrogen receptor (ER) modulators containing various hydrophobic bent-core structures |
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| Institution: | 1. Fujian Key Laboratory of Polymer Materials, College of Materials Science and Engineering, Fujian Normal University, Fuzhou 350007, Fujian, China;2. College of Resources and Chemical Engineering, San Ming University, San Ming 365007, China;1. Department of Chemistry, University of New Hampshire, Parsons Hall, 23 Academic Way, Durham, NH 03824-3598, United States;2. Department of Chemistry, University of California San Diego, La Jolla, CA 92093, United States;1. Department of Chemistry, Saint Louis University, St Louis, Missouri, USA;2. Geriatrics Research Education and Clinical Center, Veterans Affairs Puget Sound Health Care System, Seattle, Washington, USA;3. Division of Gerontology and Geriatric Medicine, Department of Medicine, University of Washington, Seattle, Washington, USA |
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| Abstract: | We previously discovered m-carborane-containing estrogen receptor (ER) modulator 4, which exhibits weak ER-agonistic and antagonistic activities in transactivation assays. With the aim of developing novel ER partial agonists, we designed and synthesized various analogues of 4 with a bent-core structure, that is, pseudo cyclic structure (5), tetrahydropyrimidinone (6), m-benzene (7), adamantane (8), and 9,10-dimethyl-m-carborane (9), in place of the m-carborane moiety. Compound 9 showed greater binding affinity than 4 in ER-binding assay using 6,7-3H]-17β-estradiol and was a more effective partial agonist than 4 in MCF-7 cell proliferation assay. It appears to be a promising candidate as a selective ER modulator (SERM). |
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| Keywords: | Bent-core structure Hydrophobic Estrogen Carborane SERM |
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