All Stories

  1. AVN-492, A Novel Highly Selective 5-HT6R Antagonist: Preclinical Evaluation

    Article • Journal of Alzheimer s Disease, June 2017, IOS Press

    Dr. ILYA OKUN

  2. Preclinical evaluation of AVN-322, novel and highly selective 5-HT6 receptor antagonist, for the treatment of Alzheimer's disease

    Article • Current Alzheimer Research, November 2016, Bentham Science Publishers

    Dr. ILYA OKUN

  3. 5-HT7 receptor antagonist with a potential to treat multiple CNS diseases

    Article • Journal of Alzheimer s Disease, July 2016, IOS Press

    Dr. ILYA OKUN

  4. Synthesis of substituted diphenyl sulfones and their structure–activity relationship with the antagonism of 5-НТ6 receptors

    Article • Bioorganic & Medicinal Chemistry, August 2013, Elsevier

    Dr. ILYA OKUN

  5. 3,6-Diamino-4-(2-halophenyl)-2-benzoylthieno[2,3- b ]pyridine-5-carbonitriles Are Selective Inhibitors of Plasmodium falciparum Glycogen Synthase Kinase-3

    Article • Journal of Medicinal Chemistry, January 2013, American Chemical Society (ACS)

    Dr. ILYA OKUN

  6. Antagonists of 5-HT6 receptors. Substituted 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 3-(phenylsulfonyl)pyrazolo[1,5-a]pyrido[4,3-d]pyrimidines—Synthesis and ‘structure–activity’ relationship

    Article • Bioorganic & Medicinal Chemistry Letters, July 2012, Elsevier

    Dr. ILYA OKUN

  7. Synthesis and Structure–Activity Relationship (SAR) of (5,7-Disubstituted 3-phenylsulfonyl-pyrazolo[1,5- a ]pyrimidin-2-yl)-methylamines as Potent Serotonin 5-HT 6 Receptor (5-HT 6 R) Antagonists

    Article • Journal of Medicinal Chemistry, December 2011, American Chemical Society (ACS)

    Dr. ILYA OKUN

  8. ChemInform Abstract: 2-Substituted 5,6-Dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: New Series of Highly Potent and Specific Serotonin 5-HT6 Receptor Antagonists.

    Article • ChemInform, June 2011, Wiley

    Dr. ILYA OKUN

  9. A Novel Synthetic Smoothened Antagonist Transiently Inhibits Pancreatic Adenocarcinoma Xenografts in a Mouse Model

    Article • PLoS ONE, June 2011, PLOS

    Dr. ILYA OKUN

  10. 2-Substituted 5,6-dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: New series of highly potent and specific serotonin 5-HT6 receptor antagonists

    Article • European Journal of Medicinal Chemistry, April 2011, Elsevier

    Dr. ILYA OKUN

  11. Synthesis and SAR of 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines as potent serotonin 5-HT6 receptor antagonists

    Article • Bioorganic & Medicinal Chemistry, February 2011, Elsevier

    Dr. ILYA OKUN

  12. (3-Phenylsulfonylcycloalkano[ e and d ]pyrazolo[1,5- a ]pyrimidin-2-yl)amines: Potent and Selective Antagonists of the Serotonin 5-HT 6 Receptor

    Article • Journal of Medicinal Chemistry, July 2010, American Chemical Society (ACS)

    Dr. ILYA OKUN

  13. Solution Phase Parallel Synthesis of Substituted 3-Phenylsulfonyl-[1,2,3]triazolo[1,5- a ]quinazolines: Selective Serotonin 5-HT 6 Receptor Antagonists

    Article • Journal of Combinatorial Chemistry, July 2010, American Chemical Society (ACS)

    Dr. ILYA OKUN

  14. Synthesis and biological study of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines as potent and selective serotonin 5-HT6 receptor antagonists

    Article • Bioorganic & Medicinal Chemistry, July 2010, Elsevier

    Dr. ILYA OKUN

  15. ChemInform Abstract: 8-Sulfonyl-Substituted Tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 Receptor Antagonists.

    Article • ChemInform, June 2010, Wiley

    Dr. ILYA OKUN

  16. Synthesis of cycloalkane-annelated 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines and their evaluation as 5-HT6 receptor antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, April 2010, Elsevier

    Dr. ILYA OKUN

  17. 8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists

    Article • European Journal of Medicinal Chemistry, February 2010, Elsevier

    Dr. ILYA OKUN

  18. Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles

    Article • Bioorganic & Medicinal Chemistry Letters, January 2010, Elsevier

    Dr. ILYA OKUN

  19. Synthesis and biological evaluation of novel γ-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, June 2009, Elsevier

    Dr. ILYA OKUN

  20. Nonpeptide Small Molecule Inhibitors of Caspases

    Article • October 2008, Taylor & Francis

    Dr. ILYA OKUN

  21. Novel aryl and heteroaryl substituted N-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,4-oxadiazole-5-carboxamides as selective GSK-3 inhibitors

    Article • Bioorganic & Medicinal Chemistry Letters, June 2008, Elsevier

    Dr. ILYA OKUN

  22. Caspase Activity Modulators as Anticancer Agents

    Article • Anti-Cancer Agents in Medicinal Chemistry, April 2008, Bentham Science Publishers

    Dr. ILYA OKUN

  23. Synthesis and Chemical Transformations of 6-(Morpholine-4-sulfonyl)-quinoline-2,3,4-tricarboxylic Acid.

    Article • ChemInform, August 2006, Wiley

    Dr. ILYA OKUN

  24. Pyrrolo[3,4-c]quinoline-1,3-diones as Potent Caspase-3 Inhibitors. Synthesis and SAR of 2-Substituted 4-Methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3,4-c]quinoline-1,3-diones.

    Article • ChemInform, April 2006, Wiley

    Dr. ILYA OKUN

  25. Synthesis and Chemical Transformations of 6‐(Morpholine‐4‐sulfonyl)‐quinoline‐2,3,4‐tricarboxylic Acid

    Article • Synthetic Communications, March 2006, Taylor & Francis

    Dr. ILYA OKUN

  26. Synthesis and Caspase-3 Inhibitory Activity of 8-Sulfonyl-1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines.

    Article • ChemInform, February 2006, Wiley

    Dr. ILYA OKUN

  27. Pyrrolo[3,4-c]Quinoline-1,3-Diones as Potent Caspase-3 Inhibitors: Synthesis and SAR of 8-Sulfamoyl-1,3-Dioxo-2,3-Dihydro-1H-Pyrrolo[3,4- c]Quinolines

    Article • Letters in Drug Design & Discovery, February 2006, Bentham Science Publishers

    Dr. ILYA OKUN

  28. NEW VARIANT OF THE PEIZINGER REACTION. SYNTHESIS AND CHEMICAL TRANSFORMATIONS OF SUBSTITUTED 2-AMINOMETHYL-QUINOLINE-3,4-DICARBOXYLIC ACIDS

    Article • Heterocyclic Communications, January 2006, De Gruyter

    Dr. ILYA OKUN

  29. Pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3,4-c]quinoline-1,3-diones

    Article • European Journal of Medicinal Chemistry, December 2005, Elsevier

    Dr. ILYA OKUN

  30. Synthesis and caspase-3 inhibitory activity of 8-sulfonyl-1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines

    Article • Il Farmaco, October 2005, Elsevier

    Dr. ILYA OKUN

  31. 1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as Potent Caspase-3 Inhibitors.

    Article • ChemInform, July 2005, Wiley

    Dr. ILYA OKUN

  32. Synthesis and Structure−Activity Relationship of 4-Substituted 2-(2-Acetyloxyethyl)-8-(morpholine- 4-sulfonyl)pyrrolo[3,4- c ]quinoline- 1,3-diones as Potent Caspase-3 Inhibitors

    Article • Journal of Medicinal Chemistry, June 2005, American Chemical Society (ACS)

    Dr. ILYA OKUN

  33. 1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors

    Article • Bioorganic & Medicinal Chemistry Letters, April 2005, Elsevier

    Dr. ILYA OKUN

  34. Efficient Optimization Strategy for Marginal Hits Active Against abl Tyrosine Kinases

    Article • Current Drug Discovery Technologies, October 2004, Bentham Science Publishers

    Dr. ILYA OKUN

  35. Property-Based Design of GPCR-Targeted Library.

    Article • ChemInform, January 2003, Wiley

    Dr. ILYA OKUN

  36. Property-Based Design of GPCR-Targeted Library

    Article • Journal of Chemical Information and Computer Sciences, November 2002, American Chemical Society (ACS)

    Dr. ILYA OKUN

  37. Serotonin Antagonist Profiling on 5HT2A and 5HT2C Receptors by Nonequilibrium Intracellular Calcium Response Using an Automated Flow-Through Fluorescence Analysis System, HT-PS® 100

    Article • SLAS DISCOVERY, June 2002, Mary Ann Liebert Inc

    Dr. ILYA OKUN

  38. High-throughput pharmocology system HT-PS 100: instrument for automated quantitative analysis of a ligand-receptor interaction based on ligand concentration-dependent functional responses in cells

    Article • April 2000, SPIE

    Dr. ILYA OKUN

  39. Functional characterization of naturally expressed G-protein-coupled receptors in mammalian cells using the automated high-throughput pharmacological system HT-PS 100

    Article • April 1999, SPIE

    Dr. ILYA OKUN

  40. The discovery and structure—activity relationships of nonpeptide, low molecular weight antagonists selective for the endothelin ETB receptor

    Article • Bioorganic & Medicinal Chemistry, December 1998, Elsevier

    Dr. ILYA OKUN

  41. 2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, August 1997, Elsevier

    Dr. ILYA OKUN

  42. Structure−Activity Relationships of N   2 -Aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as Selective Endothelin Receptor-A Antagonists 1

    Article • Journal of Medicinal Chemistry, May 1997, American Chemical Society (ACS)

    Dr. ILYA OKUN

  43. Discovery of TBC11251, a Potent, Long Acting, Orally Active Endothelin Receptor-A Selective Antagonist 1

    Article • Journal of Medicinal Chemistry, May 1997, American Chemical Society (ACS)

    Dr. ILYA OKUN

  44. New methods to mimic nature in high-throughput screening

    Article • Nature Biotechnology, March 1997, Nature

    Dr. ILYA OKUN

  45. Search for surrogates: A study of endothelin receptor antagonist structure activity relationships

    Article • Bioorganic & Medicinal Chemistry Letters, January 1997, Elsevier

    Dr. ILYA OKUN

  46. Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, January 1997, Elsevier

    Dr. ILYA OKUN

  47. Thiophenesulfonamides as endothelin receptor antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, November 1996, Elsevier

    Dr. ILYA OKUN

  48. Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists

    Article • Bioorganic & Medicinal Chemistry Letters, October 1996, Elsevier

    Dr. ILYA OKUN