| PubMed |
Abstract |
RScore(About this table) |
| 14613328 |
Cogan PS, Koch TH: Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate. J Med Chem. 2003 Nov 20;46(24):5258-70.
Relative binding affinity of the tethers bound to the targeting group for human androgen receptor were measured using a (3) H-Mibolerone competition assay and varied from 18% of nilutamide binding for the butynediol-based linear region to less than 1% for one of the piperazine derivatives. |
35(0,1,1,5) |
Details |
| 16420057 |
Kinoyama I, Taniguchi N, Toyoshima A, Nozawa E, Kamikubo T, Imamura M, Matsuhisa A, Samizu K, Kawanimani E, Niimi T, Hamada N, Koutoku H, Furutani T, Kudoh M, Okada M, Ohta M, Tsukamoto S: (+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl) phenyl]-2,5-dimethyl-N-[6-(trifl uoromethyl) pyridin-3- yl] piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist. J Med Chem. 2006 Jan 26;49(2):716-26.
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32(0,1,1,2) |
Details |
| 19143029 |
Liu CM, Lo YC, Tai MH, Wu BN, Wu WJ, Chou YH, Chai CY, Huang CH, Chen IJ: Piperazine-designed alpha 1A/alpha 1D-adrenoceptor blocker KMUP-1 and doxazosin provide down-regulation of androgen receptor and PSA in prostatic LNCaP cells growth and specifically in xenografts. Prostate. 2009 May 1;69(6):610-23.
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7(0,0,1,2) |
Details |
| 15516756 |
Kinoyama I, Taniguchi N, Yoden T, Koutoku H, Furutani T, Kudoh M, Okada M: Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists. Chem Pharm Bull. 2004 Nov;52(11):1330-3.
Among them, 4-[4-cyano-(3-trifluoromethyl) phenyl]-N-(4-fluorophenyl) piperazine-1-carbo xamide (22; YM-92088) exhibited a potent AR antagonistic activity with an IC (50) value of 0.47 microM in the reporter assay, which is more potent than bicalutamide (4) which has an IC (50) value of 0.89 microM. |
1(0,0,0,1) |
Details |