New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g]quinolinone
摘要:
A series of 2(1H)-pyrrolidino [3,2-g]quinolinones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g]quinolinone, displayed moderate interaction with hAR, but more substituted analogues, particularly 6,7-disubstituted compounds, were potent hAR agonists in vitro. (C) 1998 Elsevier Science Ltd. All rights reserved.
Compounds having the formula I wherein R
2
, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
Squarylium dyes with improved design flexibility via functionalization thereof thereby yielding desirable photophysical, solubility, thermal stability, and/or light stability properties, for example. The resulting dyes are useful in optical filters and as fluorescent indicators, for example.