Effect of a 17alpha-(3-hydroxypropyl)-17beta-acetyl substituent pattern on the glucocorticoid and progestin receptor binding of 11beta-arylestra-4,9-dien-3-ones.
[structure: see text]. Replacing the 17alpha-acetoxy substituent in an antiprogestational 17beta-acetyl-11beta-arylestra-4,9-dien-3-one by 3-hydroxypropyl significantly diminished glucocorticoid receptor binding with little effect on progestin receptor binding.
Chemistry and Life Sciences, Research Triangle Institute, Research Triangle Park, North Carolina 27709-2194, USA. cec@rti.org
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Cook
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Lee
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Kepler
D000818:Animals; D004963:Estrenes / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D005938:Glucocorticoids / Q000037:antagonists & inhibitors*; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D011372:Progestins / Q000037:antagonists & inhibitors*; D011817:Rabbits; D011965:Receptors, Glucocorticoid / Q000737:chemistry / Q000378:metabolism*; D011980:Receptors, Progesterone / Q000737:chemistry / Q000378:metabolism*
D004963:Estrenes; D005938:Glucocorticoids; D008024:Ligands; D011372:Progestins; C117799:RTI 3021-012; D011965:Receptors, Glucocorticoid; D011980:Receptors, Progesterone