159799-45-8Relevant academic research and scientific papers
1-arylsulphonyl, arylcarbonyl and 1-arylphosphonyl-3-phenyl-1,4,5,6-tetrahydropyridazines
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, (2008/06/13)
Disclosed are progestin agonists having the following formula: STR1 W is absent or --CH=CH--; R1 are independently selected from the group consisting of halogen, --CF3, and NO2, or both R1 may be joined to form a bi-radical which is --CH=CHCH=CH--; R3 are independently selected from the group consisting of hydrogen, C1-6 branched or linear alkyl, halogen and --CF3, with the proviso that R3 at the 3-position must be H where R3 at the 4-position is H, or both R3 may be joined to form a bi-radical selected from the group consisting of --CH=CHCH=CH--, --C(NC1-4 alkyl2)=CHCH=CH-- and --(CH2)4 --; R5 is selected from the group consisting of H and Me; with the proviso that only one of R1 and R3 forms the fused bi-radical; and the stereoisomers.
Nonsteroidal Progesterone Receptor Ligands. 2. High-Affinity Ligands with Selectivity for Bone Cell Progesterone Receptors
Combs, Donald W.,Reese, Kimberly,Cornelius, Lyndon A. M.,Gunnet, Joseph W.,Cryan, Ellen V.,et al.
, p. 4880 - 4884 (2007/10/03)
A novel series of nonsteroidal heterocycles was discovered which display cell-type selective, high-affinity (nanomolar) binding to the progesterone receptors from TE85 osteosarcoma cells but > 1 μM binding affinity to the progesterone receptors from T47D and ZR75 human breast carcinpma cells.Structure-activity relationships were developed for a set of these compounds, and a representative analog 1-(3,4-dichlorobenzoyl)-3-phenyl-1,4,5,6-tetrahydropyridazine (1i, RWJ 25333) was chosen for further evaluation.RWJ 25333 stimulated the in vitro proliferation of human osteoblast-like cells but not human breast cells.
