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Recent Scientific Publications

2015

  • "Residence time and kinetic efficiency analysis of extracellular signal-regulated kinase 2 inhibitors" Anal Biochem. 2015 Mar 15;473:46-52. Epub 2014 Dec 20 | Pubmed
  • "Integrated Cross-Coupling Strategy for an α-Carboline-Based Aurora B Kinase Inhibitor" J Org Chem. 2015 Feb 6;80(3):1564-8. Epub 2015 Jan 23 | Pubmed
  • "Antitumor Activity of the MEK Inhibitor TAK-733 against Melanoma Cell Lines and Patient-Derived Tumor Explants" Mol Cancer Ther. 2015 Feb;14(2):317-25. Epub 2014 Nov 5 | Pubmed

2014

  • "High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875" Nature (2014) Epub 20 Jul 2014 | Pubmed
  • "A Fragment-Based Approach to Identifying S-Adenosyl-l-methionine -Competitive Inhibitors of Catechol O-Methyl Transferase (COMT)" J Med Chem. 2014 Jun 26;57(12):5459-63. Epub 2014 Jun 4 | Pubmed
  • "Preparative Two-Dimensional Liquid Chromatography / Mass Spectrometry (2D LC-LC/MS) for the Purification of Complex Pharmaceutical Samples" J Chromatogr A. 2014 Jan 10;1324:86-95. Epub 2013 Nov 25 | Pubmed
  • "Preclinical FLT-PET and FDG-PET imaging of tumor response to the multi-targeted Aurora B kinase inhibitor, TAK-901" Nucl Med Biol. 2014 Feb;41(2):148-54. Epub 2013 Nov 15 | Pubmed

2013

  • "Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives" J Med Chem. 2013 Aug 22;56(16):6478-94.Epub 2013 Aug 1 | Pubmed
  • "Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells" Bioorg Med Chem. 2013 Oct 12.[Epub ahead of print] | Pubmed
  • "Design, stereoselective synthesis, and biological evaluation of novel tri-cyclic compounds as inhibitor of apoptosis proteins (IAP) antagonists" Bioorg Med Chem. 2013 Sep 15;21(18):5725-37. Epub 2013 Jul 18 | Pubmed
  • "Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors" Bioorg Med Chem Lett, 2013, Aug 15; 23 (16): 4501-4505 | Pubmed
  • "Development of a Practical Synthesis of a TORC1/2 Inhibitor: A Scalable Application of Memory of Chirality" Org. Process Res. Dev., Publication Date (Web): 31 Mar 2013
  • "Design, Synthesis and SAR of Novel Glucokinase Activators" Bioorg Med Chem Lett. 2013 Apr 1;23(7):2166-71. Epub 2013 Feb 4 | Pubmed
  • "Biological Characterization of TAK-901, an Investigational, Novel, Multi-Targeted Aurora B Kinase Inhibitor" Mol Cancer Ther. 2013 Apr;12(4):460-70. Epub 2013 Jan 28. | Pubmed
  • "Structure-based discovery of cellular-active allosteric inhibitors of FAK." Bioorg Med Chem Lett. 2013 Mar 15;23(6):1779-85. Epub 2013 Jan 26. | Pubmed
  • "Discovery and characterization of novel allosteric FAK inhibitors" Eur J Med Chem. 2013 Mar;61:49-60. Epub 2012 Jun 26 | Pubmed
  • "Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1)" Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. Epub 2013 Feb 27| Pubmed
  • "Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimetic." J Med Chem. 2013 Feb 14;56(3):1228-46. Epub 2013 Jan 29. | Pubmed

2012

  • "A potent anti-HB-EGF monoclonal antibody inhibits cancer cell proliferation and multiple angiogenic activities of HB-EGF" PLoS One. 2012;7(12):e51964. Epub 2012 Dec 14 | Pubmed
  • "Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors" Bioorg Med Chem. 2013 Jan 1;21(1):28-41. Epub 2012 Nov 15 | Pubmed
  • "Chemical informatics-Using protein shape descriptors in structure based drug design" in Methods in Molecular Biology, Structure Based Drug Design (ed. Leslie Tari) Humana Press, DOI 10.1007/978-1-61779-520-6, Chapter 9 2012;841:235-50 | Pubmed
  • "X-Ray Sources and High-Throughput Data Collection Methods" in Methods in Molecular Biology, Structure Based Drug Design (ed. Leslie Tari) Humana Press, DOI 10.1007/978-1-61779-520-6, Chapter 5 2012;841:93-141 | Pubmed
  • "Protein Crystallization Methods" in Methods in Molecular Biology, Structure Based Drug Design (ed. Leslie Tari) Humana Press, DOI 10.1007/978-1-61779-520-6, Chapter 4, 2012;841:67-91 | Pubmed
  • "Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors" Volume 22, Issue 21, 1 November 2012, Pages 6628-6631 | Pubmed
  • "Biacore surface matrix effects on the binding kinetics and affinity of an antigen/antibody complex" Anal Biochem. 2012 Oct 1;429(1):58-69. Epub 2012 Jul 2 | Pubmed
  • "Conformation-specific effects of Raf kinase inhibitors" J Med Chem. 2012 Sep 13;55(17):7332-41 Epub 2012 Aug 3 | Pubmed
  • "Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives." Bioorg Med Chem. 2012 Sep 15;20(18):5600-15. Epub 2012 Jul 23. | Pubmed
  • "Structure-Activity Relationships and key Structural Feature of Pyridyloxybenzene-Acylsulfonamides as New Potent and Selective Peroxisome Proliferator-Activated Receptor (PPAR) γ Partial Agonists" Bioorg Med Chem. 2012 May 15;20(10):3332-58. Epub 2012 Mar 23. | Pubmed
  • "Design and Synthesis of Orally Available MEK Inhibitors with Potent in vivo Antitumor Efficacy" Bioorg. Med. Chem. Lett 2012 Apr 1; 22(7): 2411-4. Epub 2012 Feb 20. | Pubmed
  • "A back-to-front fragment-based drug design search strategy targeting the dfg-out pocket of protein tyrosine kinases" Acs Med.Chem.Lett. (2012) 3 p.342. " Acs Med.Chem.Lett. (2012) 3 p.342. (not in pubmed).
  • "Design and Synthesis of Novel DFG-out RAF/Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) Inhibitors: (I) Exploration of [5,6]-Fused Bicyclic Scaffolds" J Med Chem. 2012 Feb 29. [Epub ahead of print] | Pubmed
  • "A New Class of Non-Thiazolidinedione Non-carboxilic acid-based Highly Selective Peroxisome Proliferator-Activated Receptor (PPAR) γ Partial Agonists: Design and Synthesis of Benzylpyrazole Acylsulfonamides" Bioorg Med Chem. 2012 Jan 15;20(2):714-33. Epub 2011 Dec 13 | Pubmed

2011

  • "TAK-960, an investigational novel, orally available, selective inhibitor of Polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple does regimens" Mol. Cancer Ther. published online 21-Dec-2011 | Pubmed
  • "Two-dimensional supercritical fluid chromatography / mass spectrometry for the enantiomeric analysis and purification of pharmaceutical samples" J. Chromatogr. A 1218 (2011) 3080-3088 | Pubmed
  • "A Strategic Approach for the Determination of Biosensor Regeneration Conditions" J Immunol Methods. 2011 Aug 31;371(1-2):165-9. Epub 2011 Jun 17 | Pubmed
  • "T7 Lytic Phage-Displayed Peptide Libraries: Construction and Diversity Characterization" Methods in Molecular Biology: Therapeutic Peptides
  • "Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2" published on line J.Biol.Chem on 30-Mar-2011. | Pubmed
  • "Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer" Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9. Epub 2011 Jan 22. | Pubmed
  • Synthetic approaches to 1,8-napthyridine-2,5-dione compounds Tetrahedron Letters 52 (2011) 477-479
  • Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IV J Med Chem. 2011 Jan 27;54(2):510-524. Epub 2010 Dec 27 | Pubmed

2010

  • "Application of Quantitative Pharmacology in the Design of First-In-Human Dosing Strategy for Development of Antibody-Based Therapeutics" AAPS J. 2010 Dec;12(4):592-601. Epub 2010 Jul 24. | Pubmed
  • "Structure-Based Design and Synthesis of Pyrrole Derivatives as MEK Inhibitors" Bioorg. Med. Chem. Lett. 2010, 20(14), 4156-4158 | Pubmed
  • "Development of a high-throughput online solid-phase extraction/tandem mass spectrometry method for cytochrome P450 inhibition screening" J Biomol Screen. 2010 Apr;15(4):447-52 | Pubmed
  • "Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity" Bioorg Med Chem Lett. 2010 May 15;20(10):3138-41 | Pubmed
  • "Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides" Bioorg Med Chem Lett. 2010 May 15;20(10):3142-5 | Pubmed
  • "Intramolecular Diels-Alder synthesis of 7-aza-alpha-carboline compounds" Tetrahedron Letters 51 (2010) 1739-1741 | ChemInform
  • "A high throughput metabolic stability screening workflow with automated assessment of data quality in pharmaceutical industry" J Chromatogr A. 2010 Mar 5;1217(10):1616-25 | Pubmed
  • "Pharmacokinetics of alogliptin when administered with food, metformin, or cimetidine: a two-phase, crossover study in healthy subjects" Int J Clin Pharmacol Ther. 2010 Jan;48(1):46-58 | Pubmed
  • "Metabolomics Based Discovery of Diagnostic Biomarkers for Onchocerciasis" PLoS Negl Trop Dis 2010, 4 (10), e834 | Pubmed