96718-82-0Relevant academic research and scientific papers
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists
Chesworth, Richard,Zawistoski, Michael P.,Lefker, Bruce A.,Cameron, Kimberly O.,Day, Robert F.,Mangano, F. Michael,Rosati, Robert L.,Colella, Stacy,Petersen, Donna N.,Brault, Amy,Lu, Bihong,Pan, Lydia C.,Perry, Pia,Ng, Oicheng,Castleberry, Tessa A.,Owen, Thomas A.,Brown, Thomas A.,Thompson, David D.,DaSilva-Jardine, Paul
, p. 2729 - 2733 (2007/10/03)
Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER α and ER β selective analogs.
Tetrahydroisoquinoline compounds as estrogen agonists/antagonists
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, (2008/06/13)
This invention relates to compounds useful for treating or preventing obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease, prostatic disease, and the like, and to pharmaceutical composition, methods, and kits comprising such compou
Antiimplantation Agents: Part II - 1,2-Diaryl-1,2,3,4-tetrahydroisoquinolines
Nagarajan, K.,Talwalker, P. K.,Kulkarni, C. L.,Shah, R. K.,Shenoy, S. J.,Prabhu, S. S.
, p. 83 - 97 (2007/10/02)
1,2-Diaryl-3,4-dihydroisoquinolinium derivatives (5) have been synthesised from N-aryl-N-aroyl-β-phenethylamines (4) and found to exhibit no antiimplantation activity in the rat whereas many of the corresponding tetrahydroisoquinolines (6) are active.Structure-activity relationships have also been studied. 1-(p-Fluorophenyl)-6-methoxy-2-phenyl-1,2,3,4-tetrahydroisoquinoline (6u) and its nor derivative (6v) are very potent, while the ortho (6g) and the meta (6n) fluoro analogues as well as the des-fluoro derivative (6d) are quite active.Extensive biological tests have been carried out on 6g.The enantiomers (+)-6p*HCl and (-)-6q*HCl of 6n have similar activity profiles as that of 6n showing no separation of antiimplantation and estrogenic properties.Diastereomeric 2-(2-methyl-2-phenethyl)-1-phenyl-1,2,3,4-tetrahydroisoquinolines (13a and 13b) show similar properties, while the tetracyclic derivative 19 is inactive. 2-Phenoxyethyl-1-phenyl-1,2,3,4-tetrahydroisoquinoline (26) shows moderate activity, but 1-(β-phenethyl)-2-phenyl-1,2,3,4-tetrahydroisoquinoline 29 is inactive.
