Amide derivatives of 9,11-seco-estra-1,3,5(10)-trien-11-oic acid as modified orally active estrogen agonists with moderate antagonistic activity

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• 作者：Negi ; Arvind Singh ; Chaturvedi ; Devdutt ; Gupta ; Atul ; Ray ; S. ; Dwivedy ; Anila ; Singh ; M.M.
• 关键词：Antiestrogens ; Estrogen antagonists ; seco Estranes ; RBA
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：January 3, 2005
• 年：2005
• 卷：15
• 期：1
• 页码：99-102
• 全文大小：268 K

文摘

Synthesis of amide derivatives of 9,11-seco-estra-1,3,5(10)-trien-11-oic acid containing alkyl and aromatic amine residues has been carried out with an aim to prepare orally active estrogen antagonists. Modification of the estradiol molecule in the form of C-seco-amide derivatives has led to their high oral absorption. Compounds 7 an n-propyl amide, 8 an n-butyl amide, and 16 a p-anisidyl amide of C-seco-estrane showed significant estrogen antagonistic activity (>20 % ), while, the majority of compounds possessed high estrogen agonistic activity on oral administration at 10mg/kg dose in rats.