Protein Information

Name estrogen receptor
Synonyms ER; ERA; ER alpha; ERalpha; ESR; ESR 1; ESR1; ESRA…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
15713417 Yang C, Xu G, Li J, Wu X, Liu B, Yan X, Wang M, Xie Y: Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1505-7.
243(3,3,3,3) Details
12014971 Gust R, Keilitz R, Schmidt K: Synthesis, structural evaluation, and estrogen receptor interaction of 2,3-diarylpiperazines. J Med Chem. 2002 May 23;45(11):2325-37.

To develop novel estrogen receptor (ER) ligands, ring-fused derivatives of the hormonally active (1R,2S)/(1S,2R)-1-(2-chloro-4-hydroxyphenyl)-2-(2,6-dichloro-4-hydroxyphen yl) ethylenediamine 4b were synthesized. (2R,3S)/(2S,3R)-2-(2-Chloro-4-hydroxyphenyl)-3-(2,6-dichloro-4-hydroxyphen yl) piperazine 4 induced ligand-dependent gene expression in MCF-7-2a cells, stably transfected with the plasmid ERE (wtc) luc and was therefore used as a lead structure.
32(0,1,1,2) Details
17001108 Muraki K, Okuya S, Tanizawa Y: Estrogen receptor alpha regulates insulin sensitivity through IRS-1 tyrosine phosphorylation in mature 3T3-L1 adipocytes. Endocr J. 2006 Dec;53(6):841-51. Epub 2006 Sep 26.

4(0,0,0,4) Details
11384241 Gust R, Keilitz R, Schmidt K: Investigations of new lead structures for the design of selective estrogen receptor modulators. J Med Chem. 2001 Jun 7;44(12):1963-70.

The selection of the heterocycles was based on theoretical consideration. (2R,3S)/(2S,3R)-2-(2-Chloro-4-hydroxyphenyl)-3-(2,6-dichloro-4-hydroxyphen yl) piperazine 2, (4R,5S)/(4S,5R)-4-(2-chloro-4-hydroxyphenyl)-5-(2,6-dichloro-4-hydroxyphen yl)-2-imidazoline 3, and 4-(2-chloro-4-hydroxyphenyl)-5-(2,6-dichloro-4-hydroxyphenyl) imidazole 4 possess a spatial structure with neighboring aromatic rings as is realized in hormonally active [1,2-diphenylethylenediamine] platinum (II) complexes.
3(0,0,0,3) Details
12856593 Wang D, Fei W, Zheng H, Weng L, Deng L: [Regulation of XW630 on estrogen receptor messenger RNA expression in osteoblasts]. Sheng Wu Yi Xue Gong Cheng Xue Za Zhi. 2003 Jun;20(2):260-3.

2(0,0,0,2) Details
11951493 Fei W, Wang D, Zheng H, Weng L: [Study of XW630 in promoting estrogen receptor expression in ovariectomized rats]. Sheng Wu Yi Xue Gong Cheng Xue Za Zhi. 2002 Jan;19(1):101-4.

2(0,0,0,2) Details
12016866 Mo Z, Jiao X, Su H, Zheng H, Weng L: [The estrogenic activities of 2-[3-estrone-N-ethyl-piperazine-methyl] tetracycline (XW630)--a new compound with anti-osteoporosis activity]. Yao Xue Xue Bao. 1998 Sep;33(9):645-9.

The affinity of XW630 with uterine estrogen receptor and its estrogenic activity were studied in this paper.
2(0,0,0,2) Details