Recent Publications by Ligand Pharmaceuticals: |
A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochrome no[3,4-f]quinoline.
The progesterone receptor plays an important role in the female... | 13th August, 2008
| Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center
| J Med Chem. 2008 Jul 10;51(13):3696-9. Epub 2008 Jun 14.
DOI Direct Link |
Discovery of structurally diverse nonsteroidal SPRMs based on a screening hit, 1,2-dihydro-2,2,4-trimethyl-6-phenylquinolinone.
Synthetic steroidal progestins and antiprogestins have been widely used... | 25th July, 2008
| Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center
| Curr Top Med Chem. 2008;8(9):766-80.
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Recent developments in the discovery of selective glucocorticoid receptor modulators (SGRMs).
Steroidal glucocorticoids are widely prescribed for the treatment of a... | 25th July, 2008
| Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive,
| Curr Top Med Chem. 2008;8(9):750-65.
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Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
Modification on a lead series of [1,4]oxazino[3,2-g]quinolin-7-ones at the... | 17th July, 2008
| Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive,
| Bioorg Med Chem Lett. 2008 May 1;18(9):2967-71. Epub 2008 Mar 23.
DOI Direct Link |
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
A novel oxachrysenone series (2) of nonsteroidal selective androgen... | 10th July, 2008
| Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center
| Bioorg Med Chem Lett. 2008 Jun 1;18(11):3431-5. Epub 2008 Apr 8.
DOI Direct Link |
LGD-5552, an antiinflammatory glucocorticoid receptor ligand with reduced side effects, in vivo.
Treatment of inflammation is often accomplished through the use of... | 11th June, 2008
| Discovery Research, Ligand Pharmaceuticals, San Diego, California 92121,
| Endocrinology. 2008 May;149(5):2080-9. Epub 2008 Jan 24.
DOI Direct Link |
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.
A series of nonsteroidal glucocorticoid receptor (GR) ligands based on a... | 3rd June, 2008
| Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive,
| Bioorg Med Chem Lett. 2008 Jun 15;18(12):3504-8. Epub 2008 May 11.
DOI Direct Link |
Cell-specific activation of the human skeletal alpha-actin by androgens.
Although it is evident that androgens increase muscle mass and strength,... | 23rd April, 2008
| Department of Research and Development, Ligand Pharmaceuticals Inc., 10275
| Endocrinology. 2008 Mar;149(3):1103-12. Epub 2007 Dec 6.
DOI Direct Link |
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
Glucocorticoids are commonly used antiinflammatory agents whose use is... | 19th January, 2008
| Discovery Research, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
| Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. Epub 2007 Nov 21.
DOI Direct Link |
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
The androgen receptor is a ligand inducible transcription factor that is... | 6th December, 2007
| Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center
| J Med Chem. 2007 Oct 18;50(21):5049-52. Epub 2007 Sep 21.
DOI Direct Link |
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
A series of androgen receptor modulators based on... | 6th December, 2007
| Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive,
| Bioorg Med Chem Lett. 2007 Oct 1;17(19):5442-6. Epub 2007 Jul 25.
DOI Direct Link |
Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.
Structure-activity relationship studies centered around 3'-substituted... | 24th October, 2007
| Discovery Research, Ligand Pharmaceuticals, Inc., 10275 Science Center
| J Med Chem. 2007 Sep 20;50(19):4699-709. Epub 2007 Aug 17.
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5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza -6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.
A series of... | 2nd October, 2007
| Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive,
| Bioorg Med Chem Lett. 2007 Aug 1;17(15):4158-62. Epub 2007 May 23.
DOI Direct Link |
Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
Recent interest in orally available androgens has fueled the search for... | 7th July, 2007
| Discovery Research, Ligand Pharmaceuticals, Inc., 10275 Science Center
| J Med Chem. 2007 May 17;50(10):2486-96. Epub 2007 Apr 17.
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Bexarotene (LGD1069, Targretin), a selective retinoid X receptor agonist, prevents and reverses gemcitabine resistance in NSCLC cells by modulating gene amplification.
Acquired drug resistance is a major obstacle in cancer therapy. As for... | 19th June, 2007
| Department of Molecular Oncology, Ligand Pharmaceuticals, Inc., San Diego,
| Cancer Res. 2007 May 1;67(9):4425-33.
DOI Direct Link |
