Clean and convenient procedure for converting primary alkyl iodides and .alpha.,.omega.-diiodoalkanes into the corresponding alkyllithium derivatives by treatment with tert-butyllithium
作者:Eiichi Negishi、Douglas R. Swanson、Christophe J. Rousset
DOI:10.1021/jo00306a022
日期:1990.9
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators
作者:Lin Zhi、Christopher M Tegley、James P Edwards、Sarah J West、Keith B Marschke、Marco M Gottardis、Dale E Mais、Todd K Jones
DOI:10.1016/s0960-894x(98)00608-8
日期:1998.12
A series of nonsteroidal human progesterone receptor (hPR) agonists, 5-alkyl 1,2-dihydrochromeno[3,4-f]quinolines, was synthesized and evaluated in cotransfection and competitive receptor binding assays. The 5-alkyl substitution was shown to be responsible for the agonist activity and substitution at C9 dramatically enhanced the potency. A number of analogues in this series showed activities similar to or better than progesterone in the cotransfection and binding assays and analogue 15 exhibited similar in vivo activity as medroxyprogesterone acetate (MPA) in murine uterine wet weight/mammary gland morphology assays. (C) 1998 Elsevier Science Ltd. All rights reserved.