J Russell Falck

Summary

Affiliation: University of Texas Southwestern Medical Center
Country: USA

Publications

  1. ncbi request reprint 11,12-epoxyeicosatrienoic acid (11,12-EET): structural determinants for inhibition of TNF-alpha-induced VCAM-1 expression
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390 9038, USA
    Bioorg Med Chem Lett 13:4011-4. 2003
  2. pmc Fe(0)-mediated synthesis of tri- and tetra-substituted olefins from carbonyls: an environmentally friendly alternative to Cr(II)
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    J Org Chem 71:8178-82. 2006
  3. pmc Cascade synthesis of (E)-2-alkylidenecyclobutanols
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    Org Lett 11:4764-6. 2009
  4. pmc 14,15-Epoxyeicosa-5,8,11-trienoic acid (14,15-EET) surrogates containing epoxide bioisosteres: influence upon vascular relaxation and soluble epoxide hydrolase inhibition
    J R Falck
    Departments of Biochemistry and Pharmacology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    J Med Chem 52:5069-75. 2009
  5. pmc Electrophilic alpha-thiocyanation of chiral and achiral N-acyl imides. A convenient route to 5-substituted and 5,5-disubstituted 2,4-thiazolidinediones
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    Bioorg Med Chem Lett 18:1768-71. 2008
  6. ncbi request reprint Synthesis and stereochemical assignment of FR252921, a promising immunosuppressant
    J Russell Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390 9038, USA
    Angew Chem Int Ed Engl 46:4527-9. 2007
  7. pmc Epoxygenase eicosanoids: synthesis of tetrahydrofuran-diol metabolites and their vasoactivity
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    Bioorg Med Chem Lett 17:2634-8. 2007
  8. pmc Stereospecific cross-coupling of alpha-(thiocarbamoyl)organostannanes with alkenyl, aryl, and heteroaryl iodides
    J R Falck
    Departments of Biochemistry and Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    J Am Chem Soc 129:790-3. 2007
  9. pmc Preparation of N-tBoc L-glutathione dimethyl and di-tert-butyl esters: versatile synthetic building blocks
    J R Falck
    Departments of Biochemistry and Pharmacology, University of Texas Southwestern Medical Center, Dallas, TX 75390 9038, USA
    Bioorg Med Chem 15:1062-6. 2007
  10. pmc Ring expansion/homologation--aldehyde condensation cascade using tert-trihalomethylcarbinols
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    Org Lett 8:4645-7. 2006

Research Grants

  1. Novel Eicosanoids: Synthesis and Function
    John Falck; Fiscal Year: 2009
  2. NOVEL EICOSANOIDS--ANALYSIS, SYNTHESIS, AND FUNCTION
    John Falck; Fiscal Year: 1999
  3. NOVEL EICOSANOIDS: ANALYSIS, SYNTHESIS, AND FUNCTION
    John Falck; Fiscal Year: 2003
  4. Novel Eicosanoids: Synthesis and Function
    John Falck; Fiscal Year: 2007
  5. EICOSANOID SYNTHESIS
    John Falck; Fiscal Year: 1993
  6. EICOSANOID SYNTHESIS
    John Falck; Fiscal Year: 1991
  7. Novel Eicosanoids: Synthesis and Function
    John R Falck; Fiscal Year: 2010

Detail Information

Publications12

  1. ncbi request reprint 11,12-epoxyeicosatrienoic acid (11,12-EET): structural determinants for inhibition of TNF-alpha-induced VCAM-1 expression
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390 9038, USA
    Bioorg Med Chem Lett 13:4011-4. 2003
    ..A series of 11,12-EET analogues were synthesized and compared using a human endothelial cell based TNF-alpha-induced VCAM-1 expression assay. The resulting data were used to map a putative recognition/binding domain for 11,12-EET...
  2. pmc Fe(0)-mediated synthesis of tri- and tetra-substituted olefins from carbonyls: an environmentally friendly alternative to Cr(II)
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    J Org Chem 71:8178-82. 2006
    ....
  3. pmc Cascade synthesis of (E)-2-alkylidenecyclobutanols
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    Org Lett 11:4764-6. 2009
    ..A facile, one-pot reaction cascade condenses 1,1,1-trichloroalkanes with alpha,beta-unsaturated ketones to unexpectedly furnish moderate to good yields of (E)-2-alkylidenecyclobutanols...
  4. pmc 14,15-Epoxyeicosa-5,8,11-trienoic acid (14,15-EET) surrogates containing epoxide bioisosteres: influence upon vascular relaxation and soluble epoxide hydrolase inhibition
    J R Falck
    Departments of Biochemistry and Pharmacology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    J Med Chem 52:5069-75. 2009
    ..5 microM, IC(50) 16 nM). These data reveal differential structural parameters for the two pharmacophores that could assist the development of potent and specific in vivo drug candidates...
  5. pmc Electrophilic alpha-thiocyanation of chiral and achiral N-acyl imides. A convenient route to 5-substituted and 5,5-disubstituted 2,4-thiazolidinediones
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    Bioorg Med Chem Lett 18:1768-71. 2008
    ..Alpha-thiocyanation of chiral N-acyl carboximides proceeds with excellent diastereoselectivity, although partial racemization occurs during subsequent cyclization...
  6. ncbi request reprint Synthesis and stereochemical assignment of FR252921, a promising immunosuppressant
    J Russell Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390 9038, USA
    Angew Chem Int Ed Engl 46:4527-9. 2007
  7. pmc Epoxygenase eicosanoids: synthesis of tetrahydrofuran-diol metabolites and their vasoactivity
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
    Bioorg Med Chem Lett 17:2634-8. 2007
    ..The THFDs potently induced relaxation of pre-contracted bovine arteries...
  8. pmc Stereospecific cross-coupling of alpha-(thiocarbamoyl)organostannanes with alkenyl, aryl, and heteroaryl iodides
    J R Falck
    Departments of Biochemistry and Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    J Am Chem Soc 129:790-3. 2007
    ..Cross-couplings proceed with retention of configuration at the alkenyl- and stannyl-substituted stereocenters...
  9. pmc Preparation of N-tBoc L-glutathione dimethyl and di-tert-butyl esters: versatile synthetic building blocks
    J R Falck
    Departments of Biochemistry and Pharmacology, University of Texas Southwestern Medical Center, Dallas, TX 75390 9038, USA
    Bioorg Med Chem 15:1062-6. 2007
    ..These l-glutathione derivatives are versatile synthetic building blocks for the preparation of S-glutathione adducts...
  10. pmc Ring expansion/homologation--aldehyde condensation cascade using tert-trihalomethylcarbinols
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA
    Org Lett 8:4645-7. 2006
    ..Acyclic tert-trihalomethylcarbinols undergo a comparable cascade of one carbon homologation-olefination...
  11. ncbi request reprint Asymmetric synthesis of the stereoisomers of 11,12,15(S)-trihydroxyeicosa-5(Z),8(Z),13(E)-trienoic acid, a potent endothelium-derived vasodilator
    J R Falck
    Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390 9038, USA
    Bioorg Med Chem Lett 14:4987-90. 2004
    ..Only 11(R),12(S),15(S)-THETA was comparable to natural material by HPLC, GC/MS, and in vitro bioassay...
  12. pmc 17(R),18(S)-epoxyeicosatetraenoic acid, a potent eicosapentaenoic acid (EPA) derived regulator of cardiomyocyte contraction: structure-activity relationships and stable analogues
    John R Falck
    Department of Biochemistry, University of Texas Southwestern, Dallas, Texas 75390, United States
    J Med Chem 54:4109-18. 2011
    ..Compared with natural material, the agonist and antagonist analogues are chemically and metabolically more robust and several show promise as templates for future development of clinical candidates...

Research Grants26

  1. Novel Eicosanoids: Synthesis and Function
    John Falck; Fiscal Year: 2009
    ..It is the long-term objective of this laboratory to identify these metabolites, develop biochemical and chemical tools to better understand their physiologic roles, and ultimately intervene pharmacologically. ..
  2. NOVEL EICOSANOIDS--ANALYSIS, SYNTHESIS, AND FUNCTION
    John Falck; Fiscal Year: 1999
    ..and (e) elucidation of the P450 active site. ..
  3. NOVEL EICOSANOIDS: ANALYSIS, SYNTHESIS, AND FUNCTION
    John Falck; Fiscal Year: 2003
    ..and (e) elucidation of the P450 active site ..
  4. Novel Eicosanoids: Synthesis and Function
    John Falck; Fiscal Year: 2007
    ..3) Develop isozyme-specific P450 inhibitors using (i) structure based rational design; (ii) computational/molecular modeling; and (iii) library screening. ..
  5. EICOSANOID SYNTHESIS
    John Falck; Fiscal Year: 1993
    ..Given the broad distribution of the new pathways in mammalian tissues, this work will have profound implications for our understanding of fatty acid metabolism and its relationship to homeostasis...
  6. EICOSANOID SYNTHESIS
    John Falck; Fiscal Year: 1991
    ..In light of the almost universal distribution of cytochrome P-450 in mammalian tissues, this work will have profound implications for our understanding of fatty acid metabolism and its relationship to homeostasis...
  7. Novel Eicosanoids: Synthesis and Function
    John R Falck; Fiscal Year: 2010
    ..It is the long-term objective of this laboratory to identify these metabolites, develop biochemical and chemical tools to better understand their physiologic roles, and ultimately intervene pharmacologically. ..