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Items: 1 to 20 of 100

1.

Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities.

Lv W, Liu J, Lu D, Flockhart DA, Cushman M.

J Med Chem. 2013 Jun 13;56(11):4611-8. doi: 10.1021/jm400364h. Epub 2013 Jun 3.

2.

Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.

Lv W, Liu J, Skaar TC, Flockhart DA, Cushman M.

J Med Chem. 2015 Mar 26;58(6):2623-48. doi: 10.1021/jm501218e. Epub 2015 Mar 9.

3.

Inhibition of cytochrome p450 enzymes by the e- and z-isomers of norendoxifen.

Liu J, Flockhart PJ, Lu D, Lv W, Lu WJ, Han X, Cushman M, Flockhart DA.

Drug Metab Dispos. 2013 Sep;41(9):1715-20. doi: 10.1124/dmd.113.052506. Epub 2013 Jul 3.

4.

The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents.

Lu WJ, Xu C, Pei Z, Mayhoub AS, Cushman M, Flockhart DA.

Breast Cancer Res Treat. 2012 May;133(1):99-109. doi: 10.1007/s10549-011-1699-4. Epub 2011 Aug 4.

PMID:
21814747
5.

Selective estrogen receptor modulators in the ruthenocene series. Synthesis and biological behavior.

Pigeon P, Top S, Vessières A, Huché M, Hillard EA, Salomon E, Jaouen G.

J Med Chem. 2005 Apr 21;48(8):2814-21.

PMID:
15828819
6.

Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.

Lv W, Liu J, Skaar TC, O'Neill E, Yu G, Flockhart DA, Cushman M.

J Med Chem. 2016 Jan 14;59(1):157-70. doi: 10.1021/acs.jmedchem.5b01677. Epub 2015 Dec 24.

7.

A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β.

Zhao LM, Jin HS, Liu J, Skaar TC, Ipe J, Lv W, Flockhart DA, Cushman M.

Bioorg Med Chem. 2016 Nov 1;24(21):5400-5409. doi: 10.1016/j.bmc.2016.08.064. Epub 2016 Aug 31.

PMID:
27647367
8.

A convenient synthesis of (Z)-4-hydroxy-N-desmethyltamoxifen (endoxifen).

Fauq AH, Maharvi GM, Sinha D.

Bioorg Med Chem Lett. 2010 May 15;20(10):3036-8. doi: 10.1016/j.bmcl.2010.03.117. Epub 2010 Apr 3.

PMID:
20400308
9.
10.

Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells.

Maximov PY, Fernandes DJ, McDaniel RE, Myers CB, Curpan RF, Jordan VC.

J Med Chem. 2014 Jun 12;57(11):4569-83. doi: 10.1021/jm500569h. Epub 2014 May 22.

11.

Synthesis of boroxifen, a nido-carborane analogue of tamoxifen.

Valliant JF, Schaffer P, Stephenson KA, Britten JF.

J Org Chem. 2002 Jan 25;67(2):383-7.

PMID:
11798307
12.

Target specific virtual screening: optimization of an estrogen receptor screening platform.

Knox AJ, Meegan MJ, Sobolev V, Frost D, Zisterer DM, Williams DC, Lloyd DG.

J Med Chem. 2007 Nov 1;50(22):5301-10. Epub 2007 Oct 5.

PMID:
17918820
13.

Development of the β-lactam type molecular scaffold for selective estrogen receptor α modulator action: synthesis and cytotoxic effects in MCF-7 breast cancer cells.

Carr M, Knox AJ, Lloyd DG, Zisterer DM, Meegan MJ.

J Enzyme Inhib Med Chem. 2016;31(sup3):117-130. Epub 2016 Aug 1.

PMID:
27476825
14.

Estrogen receptor modulators: identification and structure-activity relationships of potent ERalpha-selective tetrahydroisoquinoline ligands.

Renaud J, Bischoff SF, Buhl T, Floersheim P, Fournier B, Halleux C, Kallen J, Keller H, Schlaeppi JM, Stark W.

J Med Chem. 2003 Jul 3;46(14):2945-57.

PMID:
12825935
15.

Novel aromatase inhibitors by structure-guided design.

Ghosh D, Lo J, Morton D, Valette D, Xi J, Griswold J, Hubbell S, Egbuta C, Jiang W, An J, Davies HM.

J Med Chem. 2012 Oct 11;55(19):8464-76. doi: 10.1021/jm300930n. Epub 2012 Sep 24.

16.

Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents.

Jordan VC.

J Med Chem. 2003 Mar 27;46(7):1081-111. Review. No abstract available.

PMID:
12646017
17.

Tamoxifen metabolites as active inhibitors of aromatase in the treatment of breast cancer.

Lu WJ, Desta Z, Flockhart DA.

Breast Cancer Res Treat. 2012 Jan;131(2):473-81. doi: 10.1007/s10549-011-1428-z. Epub 2011 Mar 9.

PMID:
21390495
18.
20.

Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor.

Lloyd DG, Hughes RB, Zisterer DM, Williams DC, Fattorusso C, Catalanotti B, Campiani G, Meegan MJ.

J Med Chem. 2004 Nov 4;47(23):5612-5.

PMID:
15509159

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