Indolo [2, 1-a] isoquinolines. Syntheses, steroid hormone receptor binding affinities, and cytostatic activity

…, MR Schneider, S Von Angerer

Index: Ambros, Reinhard; Schneider, Martin R.; Angerer, Silvia von Journal of Medicinal Chemistry, 1990 , vol. 33, # 1 p. 153 - 160

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Citation Number: 34

Abstract

A number of acetoxy-substituted 5, 6-dihydroindolo [2, la] is3quinolines were synthesized and tested for binding affinity for steroid hormone receptors. All of the derivatives bind to the estrogen receptor with RBA values ranging from 1.5 to 17 (170-estradiol= 100). Some of them show binding affinities for the androgen receptor as well. In the mouse uterine weight test, the tetracycles proved to be weak estrogens with partial antagonistic activity. All of the ...