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Items: 1 to 20 of 97

1.

Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.

Salvati ME, Balog A, Shan W, Wei DD, Pickering D, Attar RM, Geng J, Rizzo CA, Gottardis MM, Weinmann R, Krystek SR, Sack J, An Y, Kish K.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):271-6.

PMID:
15603938
2.

Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.

Salvati ME, Balog A, Wei DD, Pickering D, Attar RM, Geng J, Rizzo CA, Hunt JT, Gottardis MM, Weinmann R, Martinez R.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):389-93.

PMID:
15603960
3.

Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.

Salvati ME, Balog A, Shan W, Rampulla R, Giese S, Mitt T, Furch JA, Vite GD, Attar RM, Jure-Kunkel M, Geng J, Rizzo CA, Gottardis MM, Krystek SR, Gougoutas J, Galella MA, Obermeier M, Fura A, Chandrasena G.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1910-5. doi: 10.1016/j.bmcl.2008.02.006. Epub 2008 Feb 8.

PMID:
18291644
4.

Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.

Guo C, Linton A, Kephart S, Ornelas M, Pairish M, Gonzalez J, Greasley S, Nagata A, Burke BJ, Edwards M, Hosea N, Kang P, Hu W, Engebretsen J, Briere D, Shi M, Gukasyan H, Richardson P, Dack K, Underwood T, Johnson P, Morell A, Felstead R, Kuruma H, Matsimoto H, Zoubeidi A, Gleave M, Los G, Fanjul AN.

J Med Chem. 2011 Nov 10;54(21):7693-704. doi: 10.1021/jm201059s. Epub 2011 Oct 7.

PMID:
21936524
5.

The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening.

Lanter JC, Fiordeliso JJ, Jiang W, Allan GF, Lai MT, Linton O, Hahn do W, Lundeen SG, Sui Z.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):123-6. Epub 2006 Sep 30.

PMID:
17071085
6.

The androgen receptor T877A mutant recruits LXXLL and FXXLF peptides differently than wild-type androgen receptor in a time-resolved fluorescence resonance energy transfer assay.

Ozers MS, Marks BD, Gowda K, Kupcho KR, Ervin KM, De Rosier T, Qadir N, Eliason HC, Riddle SM, Shekhani MS.

Biochemistry. 2007 Jan 23;46(3):683-95.

PMID:
17223690
7.
8.

Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.

Hamann LG, Higuchi RI, Zhi L, Edwards JP, Wang XN, Marschke KB, Kong JW, Farmer LJ, Jones TK.

J Med Chem. 1998 Feb 12;41(4):623-39.

PMID:
9484511
9.

Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.

Hamann LG, Manfredi MC, Sun C, Krystek SR Jr, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1860-4. Epub 2007 Jan 27.

PMID:
17292608
10.
11.

Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.

Handratta VD, Vasaitis TS, Njar VC, Gediya LK, Kataria R, Chopra P, Newman D Jr, Farquhar R, Guo Z, Qiu Y, Brodie AM.

J Med Chem. 2005 Apr 21;48(8):2972-84.

PMID:
15828836
12.

A novel steroidal antiandrogen targeting wild type and mutant androgen receptors.

Andrieu T, Bertolini R, Nichols SE, Setoud R, Frey FJ, Baker ME, Frey BM.

Biochem Pharmacol. 2011 Dec 1;82(11):1651-62. doi: 10.1016/j.bcp.2011.08.020. Epub 2011 Sep 1.

PMID:
21907706
13.

Novel non-steroidal/non-anilide type androgen antagonists with an isoxazolone moiety.

Ishioka T, Kubo A, Koiso Y, Nagasawa K, Itai A, Hashimoto Y.

Bioorg Med Chem. 2002 May;10(5):1555-66.

PMID:
11886817
14.

3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.

Crawforth J, Goodacre S, Maxey R, Bourrain S, Patel S, Marwood R, O'Connor D, Herbert R, Hutson P, Rowley M.

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2701-3.

PMID:
11133072
15.

Antiandrogenic effects of novel androgen synthesis inhibitors on hormone-dependent prostate cancer.

Long BJ, Grigoryev DN, Nnane IP, Liu Y, Ling YZ, Brodie AM.

Cancer Res. 2000 Dec 1;60(23):6630-40.

16.

Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives.

Ng RA, Guan J, Alford VC Jr, Lanter JC, Allan GF, Sbriscia T, Linton O, Lundeen SG, Sui Z.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):784-8. Epub 2006 Oct 28.

PMID:
17095226
17.

Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome.

Goto T, Ohta K, Fujii S, Ohta S, Endo Y.

J Med Chem. 2010 Jul 8;53(13):4917-26. doi: 10.1021/jm100316f.

PMID:
20521823
18.

Antitumor agents. 217. Curcumin analogues as novel androgen receptor antagonists with potential as anti-prostate cancer agents.

Ohtsu H, Xiao Z, Ishida J, Nagai M, Wang HK, Itokawa H, Su CY, Shih C, Chiang T, Chang E, Lee Y, Tsai MY, Chang C, Lee KH.

J Med Chem. 2002 Nov 7;45(23):5037-42.

PMID:
12408714
19.

Design and synthesis of novel androgen receptor antagonists with sterically bulky icosahedral carboranes.

Goto T, Ohta K, Suzuki T, Ohta S, Endo Y.

Bioorg Med Chem. 2005 Dec 1;13(23):6414-24. Epub 2005 Aug 15.

PMID:
16099660
20.

Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists.

Guo C, Pairish M, Linton A, Kephart S, Ornelas M, Nagata A, Burke B, Dong L, Engebretsen J, Fanjul AN.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2572-8. doi: 10.1016/j.bmcl.2012.01.116. Epub 2012 Feb 7.

PMID:
22377517

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