Longqin Hu

Summary

Affiliation: Rutgers University
Country: USA

Publications

  1. pmc Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction
    Longqin Hu
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 23:3039-43. 2013
  2. doi request reprint Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs
    Longqin Hu
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 21:3986-91. 2011
  3. ncbi request reprint Design, synthesis, and biological evaluation of cyclic and acyclic nitrobenzylphosphoramide mustards for E. coli nitroreductase activation
    Yongying Jiang
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, 08854, USA
    J Med Chem 49:4333-43. 2006
  4. ncbi request reprint Nitroaryl phosphoramides as novel prodrugs for E. coli nitroreductase activation in enzyme prodrug therapy
    Longqin Hu
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, New Jersey 08854, USA
    J Med Chem 46:4818-21. 2003
  5. doi request reprint Synthesis and stereochemical preference of peptide 4-aminocyclophosphamide conjugates as potential prodrugs of phosphoramide mustard for activation by prostate-specific antigen (PSA)
    Yongying Jiang
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 19:2587-90. 2009
  6. ncbi request reprint Nitrobenzocyclophosphamides as potential prodrugs for bioreductive activation: synthesis, stability, enzymatic reduction, and antiproliferative activity in cell culture
    Zhuorong Li
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Bioorg Med Chem 11:4171-8. 2003
  7. ncbi request reprint Phenylalanyl-aminocyclophosphamides as model prodrugs for proteolytic activation: synthesis, stability, and stereochemical requirements for enzymatic cleavage
    Yongying Jiang
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 17:517-21. 2007
  8. pmc Optimization of fluorescently labeled Nrf2 peptide probes and the development of a fluorescence polarization assay for the discovery of inhibitors of Keap1-Nrf2 interaction
    Daigo Inoyama
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ, USA
    J Biomol Screen 17:435-47. 2012
  9. doi request reprint 3-Aminoxypropionate-based linker system for cyclization activation in prodrug design
    Yiyu Ge
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 19:941-4. 2009
  10. doi request reprint Design of anticancer prodrugs for reductive activation
    Yu Chen
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Med Res Rev 29:29-64. 2009

Collaborators

Detail Information

Publications21

  1. pmc Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction
    Longqin Hu
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 23:3039-43. 2013
    ..The stereospecific nature of binding between (SRS)-5 and Keap1 as well as the preliminary but tractable structure-activity relationships support its use as a lead for our ongoing optimization...
  2. doi request reprint Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs
    Longqin Hu
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 21:3986-91. 2011
    ..coli nitroreductase-expressing cells and in trypanosomatids expressing endogenous nitroreductases...
  3. ncbi request reprint Design, synthesis, and biological evaluation of cyclic and acyclic nitrobenzylphosphoramide mustards for E. coli nitroreductase activation
    Yongying Jiang
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, 08854, USA
    J Med Chem 49:4333-43. 2006
    ..The low IC(50), high selectivity, and good bystander effects of nitrobenzylphosphoramide mustards in NTR-expressing cells suggest that they could be used in combination with E. coli nitroreductase in enzyme prodrug therapy...
  4. ncbi request reprint Nitroaryl phosphoramides as novel prodrugs for E. coli nitroreductase activation in enzyme prodrug therapy
    Longqin Hu
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, New Jersey 08854, USA
    J Med Chem 46:4818-21. 2003
    ..This is about 100x more active and 27x more selective than CB1954 (1). The superior activity was attributed to its better substrate activity (k(cat)/K(m) 19x better than 1) and/or excellent cytotoxicity of phosphoramide mustard released...
  5. doi request reprint Synthesis and stereochemical preference of peptide 4-aminocyclophosphamide conjugates as potential prodrugs of phosphoramide mustard for activation by prostate-specific antigen (PSA)
    Yongying Jiang
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 19:2587-90. 2009
    ..These results clarified the stereochemical requirements of PSA on the peptide conjugates of 4-NH(2)-CPA and demonstrated the potential of these conjugates as potential PSA-activated prodrugs targeting prostate cancer...
  6. ncbi request reprint Nitrobenzocyclophosphamides as potential prodrugs for bioreductive activation: synthesis, stability, enzymatic reduction, and antiproliferative activity in cell culture
    Zhuorong Li
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Bioorg Med Chem 11:4171-8. 2003
    ..Compounds 6a and 6c represent a new structure type for reductive activation and a lead for further modification in the development of better analogues with improved selective toxicity to be used in gene-directed enzyme prodrug therapy...
  7. ncbi request reprint Phenylalanyl-aminocyclophosphamides as model prodrugs for proteolytic activation: synthesis, stability, and stereochemical requirements for enzymatic cleavage
    Yongying Jiang
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 17:517-21. 2007
    ..These results suggest the feasibility of using peptide-conjugated cis-(4R)-4-NH2-CPA as potential prodrugs for proteolytic activation in tumor tissues...
  8. pmc Optimization of fluorescently labeled Nrf2 peptide probes and the development of a fluorescence polarization assay for the discovery of inhibitors of Keap1-Nrf2 interaction
    Daigo Inoyama
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ, USA
    J Biomol Screen 17:435-47. 2012
    ....
  9. doi request reprint 3-Aminoxypropionate-based linker system for cyclization activation in prodrug design
    Yiyu Ge
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 19:941-4. 2009
    ....
  10. doi request reprint Design of anticancer prodrugs for reductive activation
    Yu Chen
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Med Res Rev 29:29-64. 2009
    ....
  11. doi request reprint N-(2,2-Dimethyl-2-(2-nitrophenyl)acetyl)-4-aminocyclophosphamide as a potential bioreductively activated prodrug of phosphoramide mustard
    Yongying Jiang
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 18:4059-63. 2008
    ..These results validated 4-aminocyclophosphamide as a prodrug form of phosphoramide mustard and suggest that compound 4 can potentially be used as a prodrug of phosphoramide mustard for bioreductive activation...
  12. pmc Small molecule modulators of Keap1-Nrf2-ARE pathway as potential preventive and therapeutic agents
    Sadagopan Magesh
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Med Res Rev 32:687-726. 2012
    ..We also discuss several aspects of Keap1-Nrf2 interaction, Nrf2-based peptide inhibitor design, and the screening assays currently used for the discovery of direct inhibitors of Keap1-Nrf2 interaction...
  13. doi request reprint Design, synthesis, and evaluation of potential prodrugs of DFMO for reductive activation
    Yanhui Yang
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA
    Bioorg Med Chem Lett 22:6583-6. 2012
    ..It was found that only modification of N(ε)-amino group of DFMO by 4-nitro-2-fluorobenzyloxycarbonyl resulted in significant trypanocidal activity and could serve as a lead for further investigation...
  14. pmc Kinetic analyses of keap1-nrf2 interaction and determination of the minimal nrf2 Peptide sequence required for keap1 binding using surface plasmon resonance
    Yu Chen
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA The Cancer Institute of New Jersey, New Brunswick, NJ 08901, USA Department of Biochemistry, University of Missouri Columbia, Columbia, MO 65211, USA
    Chem Biol Drug Des 78:1014-21. 2011
    ..These results suggest that the minimal Nrf2 peptide sequence required for Keap1 binding is the 9mer sequence of LDEETGEFL...
  15. ncbi request reprint Efficient amidation from carboxylic acids and azides via selenocarboxylates: application to the coupling of amino acids and peptides with azides
    Xinghua Wu
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, New Jersey 08854, USA
    J Org Chem 72:765-74. 2007
    ..It provides an attractive alternative method to the conventional acylation of amines when an amide bond needs to be formed without going through an amine intermediate...
  16. doi request reprint In Vitro and in Vivo Anti-inflammatory Effects of a Novel 4,6-Bis ((E)-4-hydroxy-3-methoxystyryl)-1-phenethylpyrimidine-2(1H)-thione
    Jong Hun Lee
    Center for Cancer Prevention Research, Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, New Jersey 08854, United States
    Chem Res Toxicol 27:34-41. 2014
    ..Thus, HPT demonstrated anti-inflammatory activity both in LPS-induced RAW 264.7 cells and TPA-stimulated mouse skin and may therefore serve as a potential anti-inflammatory agent. ..
  17. pmc A novel high-yield synthesis of aminoacyl p-nitroanilines and aminoacyl 7-amino-4-methylcoumarins: Important synthons for the synthesis of chromogenic/fluorogenic protease substrates
    Xinghua Wu
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, New Jersey 08854
    Beilstein J Org Chem 7:1030-5. 2011
    ....
  18. pmc Anti-NF-kappaB and anti-inflammatory activities of synthetic isothiocyanates: effect of chemical structures and cellular signaling
    Auemduan Prawan
    Center for Cancer Prevention Research, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, United States
    Chem Biol Interact 179:202-11. 2009
    ..Taken together, our findings provide the possibility that synthetic ITC analogs might have promising cancer chemopreventive potential, based on their stronger anti-NF-kappaB and anti-inflammatory activities, than the natural ITCs...
  19. ncbi request reprint 5'-(2-Nitrophenylalkanoyl)-2'-deoxy-5-fluorouridines as potential prodrugs of FUDR for reductive activation
    Bin Liu
    Department of Pharmaceutical Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Bioorg Med Chem 11:3889-99. 2003
    ..The fact that the amino intermediates cyclized easily to release the incorporated drug FUDR suggests the feasibility of using peptide-linked acyl 2-aminophenylalkanoic acid esters as potential prodrugs for proteolytic activation...
  20. doi request reprint Peptide conjugates of 4-aminocyclophosphamide as prodrugs of phosphoramide mustard for selective activation by prostate-specific antigen (PSA)
    Yongying Jiang
    Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA
    Bioorg Med Chem 21:7507-14. 2013
    ..5 and 12h, respectively. These results indicate a potential of the conjugate 3 as an anticancer prodrug of phosphoramide mustard for selective PSA activation...
  21. ncbi request reprint Prodrugs: effective solutions for solubility, permeability and targeting challenges
    Longqin Hu
    Rutgers, The State University of New Jersey, Department of Pharmaceutical Chemistry, College of Pharmacy, 08854 8020, USA
    IDrugs 7:736-42. 2004
    ..Several case studies were presented including improved pharmaceutical products in the clinic and at various stages of development...