L Zhi

Summary

Affiliation: Ligand Pharmaceuticals
Country: USA

Publications

  1. ncbi request reprint An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate
    Jeffrey N Miner
    Research Development, Ligand Pharmaceuticals Inc, San Deigo, California 92121, USA
    Endocrinology 148:363-73. 2007
  2. ncbi request reprint Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators
    Esther Martinborough
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 50:5049-52. 2007
  3. ncbi request reprint 5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists
    L Zhi
    Department of Medicinal Chemistry, Ligand Pharmaceuticals, Inc, San Diego, California 92121, USA
    J Med Chem 41:291-302. 1998
  4. ncbi request reprint 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 46:4104-12. 2003
  5. ncbi request reprint Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 13:2075-8. 2003
  6. ncbi request reprint Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 13:2071-4. 2003
  7. ncbi request reprint Discovery of structurally diverse nonsteroidal SPRMs based on a screening hit, 1,2-dihydro-2,2,4-trimethyl-6-phenylquinolinone
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, CA 92121, USA
    Curr Top Med Chem 8:766-80. 2008
  8. ncbi request reprint Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines
    L Zhi
    Ligand Pharmaceuticals, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 10:415-8. 2000
  9. ncbi request reprint Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists
    J P Edwards
    Departments of Medicinal Chemistry and Endocrine Research, Ligand Pharmaceuticals Inc, San Diego, California 92121, USA
    J Med Chem 41:2779-85. 1998
  10. ncbi request reprint Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines
    L G Hamann
    Department of Medicinal Chemistry, Ligand Pharmaceuticals, Inc, San Diego, California 92121, USA
    J Med Chem 41:623-39. 1998

Collaborators

  • L G Hamann
  • Jon Rosen
  • Jeffrey N Miner
  • Neelakandha S Mani
  • Feng Wang
  • J P Edwards
  • Tao Jiang
  • Stacie S Canan Koch
  • Wan Ching Yen
  • Luc J Farmer
  • Steven L Roach
  • Keith B Marschke
  • Francisco J Lopez
  • Arjan van Oeveren
  • Robert I Higuchi
  • Andres Negro-Vilar
  • Yun Oliver Long
  • Shuo Zhao
  • Robert J Ardecky
  • Dale E Mais
  • Donald S Karanewsky
  • Yixing Shen
  • Thomas R Caferro
  • Andrew R Hudson
  • Esther Martinborough
  • William T Schrader
  • Bijan Pedram
  • Min Wu
  • Deepa Rungta
  • Marquis L Cummings
  • Thomas L S Lau
  • William Y Chang
  • Esther A Martinborough
  • Dean P Phillips
  • Yongkai Li
  • Todd K Jones
  • Mark E Adams
  • E Adam Kallel
  • Christopher M Tegley
  • Mark D Leibowitz
  • Louise De Grandpre
  • Khalid Benbatoul
  • Bruce Bebo
  • Sha Liu
  • Pieter M Verbost
  • Keith Marschke
  • Marinus B Groen
  • Humberto O Viveros
  • Jean Yen
  • Jyun Hung Chen
  • Lino J Valdez
  • Charlotte P Deckhut
  • Sarah West
  • Barbara A Pio
  • Mehrnoush Motamedi
  • William Chang
  • Eric G Vajda
  • Reid P Bissonnette
  • Peter J Rix
  • Anthony W Thompson
  • Charlotte Deckhut
  • Kristen L Arienti
  • Angie Vassar
  • William W Lamph
  • John S Tyhonas
  • Thomas L Lau
  • Adam Kallel
  • Catherine J Gharbaoui
  • Catalina Cuervo
  • O Humberto Viveros
  • Mehrnouch Motamedi

Detail Information

Publications26

  1. ncbi request reprint An orally active selective androgen receptor modulator is efficacious on bone, muscle, and sex function with reduced impact on prostate
    Jeffrey N Miner
    Research Development, Ligand Pharmaceuticals Inc, San Deigo, California 92121, USA
    Endocrinology 148:363-73. 2007
    ..Taken together, these results suggest that orally active, nonsteroidal selective androgen receptor modulators may be useful therapeutics for enhancing muscle, bone, and sexual function...
  2. ncbi request reprint Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators
    Esther Martinborough
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 50:5049-52. 2007
    ..The compound also improved bone strength in a rat model of post-menopausal osteoporosis...
  3. ncbi request reprint 5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists
    L Zhi
    Department of Medicinal Chemistry, Ligand Pharmaceuticals, Inc, San Diego, California 92121, USA
    J Med Chem 41:291-302. 1998
    ..41-3.6 nM) than progesterone (Ki = 3.5 nM). Three representative analogues (13, 15, and 24) demonstrated in vivo activities in mammary gland morphology/uterine wet weight assay in ovariectomized rats...
  4. ncbi request reprint 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 46:4104-12. 2003
    ....
  5. ncbi request reprint Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 13:2075-8. 2003
    ..A number of potent analogues were identified by modification of the substituents at the D-ring...
  6. ncbi request reprint Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 13:2071-4. 2003
    ..A number of orally available highly potent nonsteroidal modulators were identified by modification of the substituents at 5-methylidene position...
  7. ncbi request reprint Discovery of structurally diverse nonsteroidal SPRMs based on a screening hit, 1,2-dihydro-2,2,4-trimethyl-6-phenylquinolinone
    Lin Zhi
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, CA 92121, USA
    Curr Top Med Chem 8:766-80. 2008
    ..This review describes medicinal chemistry progress of multiple nonsteroidal SPRM series based on a screening hit, 1,2-dihydro-2,2,4-trimethyl-6-phenylquinolinone...
  8. ncbi request reprint Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines
    L Zhi
    Ligand Pharmaceuticals, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 10:415-8. 2000
    ..Synthesis and biological evaluation of 6-thiophene 1,2-dihydro or 1,2,3,4-tetrahydroquinoline derivatives resulted in a number of potent nonsteroidal antiprogestins...
  9. ncbi request reprint Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists
    J P Edwards
    Departments of Medicinal Chemistry and Endocrine Research, Ligand Pharmaceuticals Inc, San Diego, California 92121, USA
    J Med Chem 41:2779-85. 1998
    ..These studies demonstrate that certain members of this class of selective progesterone receptor modulators display encouraging and potentially useful tissue-selective progestational effects...
  10. ncbi request reprint Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines
    L G Hamann
    Department of Medicinal Chemistry, Ligand Pharmaceuticals, Inc, San Diego, California 92121, USA
    J Med Chem 41:623-39. 1998
    ..Molecules based on this series of compounds have the potential to provide unique and effective clinical opportunities for treatment of prostate cancer and other androgen-dependent diseases...
  11. ncbi request reprint Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma
    Andrew R Hudson
    Discovery Research, Ligand Pharmaceuticals, Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 50:4699-709. 2007
    ..In vivo evaluation of these compounds utilizing a 28 day mouse tumor xenograft model demonstrated efficacy equal to dexamethasone in the reduction of tumor volume...
  12. pmc Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile
    Jeffrey N Miner
    Discovery Research, Ligand Pharmaceuticals, San Diego, CA 92121, USA
    Proc Natl Acad Sci U S A 104:19244-9. 2007
    ..This class of nonsteroidal, GR-dependent antiinflammatory drugs may offer a safer alternative to steroidal glucocorticoids in the treatment of inflammatory disease...
  13. doi request reprint LGD-5552, an antiinflammatory glucocorticoid receptor ligand with reduced side effects, in vivo
    Francisco J Lopez
    Discovery Research, Ligand Pharmaceuticals, San Diego, California 92121, USA
    Endocrinology 149:2080-9. 2008
    ....
  14. doi request reprint Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity
    Yun Oliver Long
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 18:2967-71. 2008
    ..The most potent analog (-)-33a exhibited full maintenance of levator ani muscle at 3mg/kg and reduced activity on ventral prostate weight in a 2-week orally-dosed and orchidectomized rat maintenance assay...
  15. doi request reprint Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones
    Shuo Zhao
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 18:3431-5. 2008
    ..In the cotransfection assay, lead compound 5d showed AR agonist activity more potent than dihydrotestosterone (DHT), whereas compound 17b was a potent antagonist similar to bicalutamide...
  16. doi request reprint Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines
    Steven L Roach
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 18:3504-8. 2008
    ..5nM) and 100- to 1000-fold selectivity over MR, PR, and AR while showing activity in an E-selectin repression assay...
  17. pmc Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones
    Robert I Higuchi
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:5442-6. 2007
    ..Compound 18h demonstrated full efficacy in the maintenance of muscle weight, at 10 mg/kg, with reduced activity in prostate weight in an in vivo model of androgen action...
  18. doi request reprint A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline
    Bijan Pedram
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 51:3696-9. 2008
    ..The compound also suppressed ovulation in monkeys, but in contrast to currently approved steroidal PR agonists, it did not suppress estradiol levels...
  19. ncbi request reprint Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid
    Luc J Farmer
    Discovery Research, Ligand Pharmaceuticals, Inc, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 13:261-4. 2003
    ..The most potent pan-agonist 5a (RAR's EC(50)=17-59 nM; RXR's EC(50)=6-14 nM) showed good antiproliferative properties in the in vitro cancer cell lines, ME 180 and RPMI 8226...
  20. ncbi request reprint Aza-retinoids as novel retinoid X receptor-specific agonists
    Luc J Farmer
    Ligand Pharmaceuticals Inc, 10255 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:2352-6. 2006
    ..Further, we have expanded the work to include azadienoic acids, which exhibited many accessible conformations leading to a better understanding of the SAR around the series...
  21. ncbi request reprint Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator
    Arjan van Oeveren
    Discovery Research, Ligand Pharmaceuticals Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 49:6143-6. 2006
    ..However, currently available androgens have many drawbacks. We identified 6-dialkylamino-4-trifluoromethylquinolin-2(1H)-ones as orally available tissue-selective androgen receptor modulators...
  22. pmc Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226
    Feng Wang
    National Laboratory of Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences, 15 Datun Road, Chaoyang District, Beijing 100101, People s Republic of China
    Acta Crystallogr Sect F Struct Biol Cryst Commun 62:1067-71. 2006
    ..It is hoped that this will aid in further explaining the selectivity of LGD2226 observed in in vitro and in vivo assays and in developing more selective and effective therapeutic agents...
  23. ncbi request reprint Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones
    Arjan van Oeveren
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:1523-6. 2007
    ..The series demonstrated selective high binding affinity to androgen receptor and potent receptor modulating activities in the cotransfection assays...
  24. ncbi request reprint Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones
    Arjan van Oeveren
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:1527-31. 2007
    ..A representative analog (9) was tested orally in a rodent model of hypogonadism and demonstrated desirable tissue selectivity...
  25. ncbi request reprint Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones
    Robert I Higuchi
    Discovery Research, Ligand Pharmaceuticals, Inc, 10275 Science Center Drive, San Diego, California 92121, USA
    J Med Chem 50:2486-96. 2007
    ..These data suggest that these compounds may be utilized as selective androgen receptor modulators or SARMs. This series represents a novel class of compounds for use in androgen replacement therapy...
  26. ncbi request reprint 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
    Robert J Ardecky
    Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:4158-62. 2007
    ..The synthesis and structure-activity relationships for this series of compounds are presented...