Maria V Papadopoulou

Summary

Publications

  1. doi request reprint Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, 2650 Ridge Ave, Evanston, IL 60201, USA Electronic address
    Bioorg Med Chem 23:6467-76. 2015
  2. doi request reprint 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, IL, USA Electronic address
    Eur J Med Chem 103:325-34. 2015
  3. pmc Nitrotriazole- and imidazole-based amides and sulfonamides as antitubercular agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, Evanston, Illinois, USA
    Antimicrob Agents Chemother 58:6828-36. 2014
  4. doi request reprint Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, IL, USA Electronic address
    Eur J Med Chem 87:79-88. 2014
  5. pmc Novel 3-nitro-1H-1,2,4-triazole-based piperazines and 2-amino-1,3-benzothiazoles as antichagasic agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, 2650 Ridge Ave, Evanston, IL 60201, USA Electronic address
    Bioorg Med Chem 21:6600-7. 2013
  6. pmc Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, Illinois, United States
    J Med Chem 55:5554-65. 2012
  7. pmc Novel 3-nitro-1H-1,2,4-triazole-based aliphatic and aromatic amines as anti-chagasic agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, Evanston, Illinois 60201, United States
    J Med Chem 54:8214-23. 2011
  8. doi request reprint Hypoxia-dependent retinal toxicity of NLCQ-1 (NSC 709257) in BALB/c mice. Comparison with tirapazamine
    Maria V Papadopoulou
    Department of Radiation Medicine, NorthShore University Healthsystem, Evanston, IL 60201, USA
    Basic Clin Pharmacol Toxicol 108:396-9. 2011
  9. doi request reprint Investigational new drug-directed, 5-day repeat dose toxicity study of 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) administered with or without Taxol in Sprague-Dawley rats
    Maria V Papadopoulou
    Department of Radiation Medicine, NorthShore University Healthsystem, Evanston, IL 60201, USA
    Basic Clin Pharmacol Toxicol 106:497-504. 2010
  10. doi request reprint Investigational new drug-directed toxicology and pharmacokinetic study of 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) in Beagle dogs
    Maria V Papadopoulou
    Department of Radiation Medicine, NorthShore University Healthsystem, Evanston, IL 60201, USA
    Basic Clin Pharmacol Toxicol 106:511-22. 2010

Detail Information

Publications31

  1. doi request reprint Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, 2650 Ridge Ave, Evanston, IL 60201, USA Electronic address
    Bioorg Med Chem 23:6467-76. 2015
    ..cruzi CYP51 and, being excellent substrates for the type I nitroreductase (NTR) which is specific to trypanosomatids, work as prodrugs and constitute a new generation of effective and more affordable antitrypanosomal agents...
  2. doi request reprint 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, IL, USA Electronic address
    Eur J Med Chem 103:325-34. 2015
    ..Working as prodrugs, 3-nitrotriazole-based piperazides were excellent substrates of trypanosomal type I nitroreductases and constitute a novel class of potentially effective and more affordable antitrypanosomal agents...
  3. pmc Nitrotriazole- and imidazole-based amides and sulfonamides as antitubercular agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, Evanston, Illinois, USA
    Antimicrob Agents Chemother 58:6828-36. 2014
    ..However, some compounds caused toxicity in uninfected macrophages. In conclusion, the classes of 3-nitrotriazole-based amides and sulfonamides merit further investigation as potential antitubercular agents. ..
  4. doi request reprint Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, IL, USA Electronic address
    Eur J Med Chem 87:79-88. 2014
    ..cruzi than the reference compound benznidazole...
  5. pmc Novel 3-nitro-1H-1,2,4-triazole-based piperazines and 2-amino-1,3-benzothiazoles as antichagasic agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, 2650 Ridge Ave, Evanston, IL 60201, USA Electronic address
    Bioorg Med Chem 21:6600-7. 2013
    ..cruzi amastigotes) from 117 to 1725 and 12 of 13 compounds were up to 39-fold more potent than the reference compound benznidazole. Detailed SARs are discussed. ..
  6. pmc Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, Illinois, United States
    J Med Chem 55:5554-65. 2012
    ..Finally, three nitrotriazoles displayed a moderate activity against the axenic form of Leishmania donovani . Therefore, 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides are potent antitrypanosomal agents...
  7. pmc Novel 3-nitro-1H-1,2,4-triazole-based aliphatic and aromatic amines as anti-chagasic agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Department of Radiation Medicine, Evanston, Illinois 60201, United States
    J Med Chem 54:8214-23. 2011
    ..b. brucei trypomastigotes with elevated TbNTR levels were hypersensitive to tested compounds. Therefore, a novel class of affordable 3-nitro-1,2,4-triazole-based compounds with antitrypanosomal activity has been identified...
  8. doi request reprint Hypoxia-dependent retinal toxicity of NLCQ-1 (NSC 709257) in BALB/c mice. Comparison with tirapazamine
    Maria V Papadopoulou
    Department of Radiation Medicine, NorthShore University Healthsystem, Evanston, IL 60201, USA
    Basic Clin Pharmacol Toxicol 108:396-9. 2011
    ..50 ± 0.04, 0.48 ± 0.03 and 0.33 ± 0.06 was determined for untreated, NLCQ-1 and TPZ-treated mice at the highest dose, respectively. Marginal retinal toxicity was observed with the lower dose of TPZ in combination with CPM...
  9. doi request reprint Investigational new drug-directed, 5-day repeat dose toxicity study of 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) administered with or without Taxol in Sprague-Dawley rats
    Maria V Papadopoulou
    Department of Radiation Medicine, NorthShore University Healthsystem, Evanston, IL 60201, USA
    Basic Clin Pharmacol Toxicol 106:497-504. 2010
    ..Daily administration of 9 (male rats) or 12 (female rats) mg/kg of NLCQ-1 1 hr after i.v. administration of Taxol (3.5 mg/kg) had no effect on Taxol-induced toxicity...
  10. doi request reprint Investigational new drug-directed toxicology and pharmacokinetic study of 4-[3-(2-nitro-1-imidazolyl)-propylamino]-7-chloroquinoline hydrochloride (NLCQ-1, NSC 709257) in Beagle dogs
    Maria V Papadopoulou
    Department of Radiation Medicine, NorthShore University Healthsystem, Evanston, IL 60201, USA
    Basic Clin Pharmacol Toxicol 106:511-22. 2010
    ..Any drug-related toxicity noted was readily reversible and not cumulative. No sex difference was detected in the susceptibility to NLCQ-1-induced toxicity...
  11. doi request reprint Nitroimidazole-based bioreductive compounds bearing a quinazoline or a naphthyridine chromophore
    Maria V Papadopoulou
    Department of Radiation Medicine, NorthShore University Health System, Evanston, IL 60201, USA
    Anticancer Drugs 20:493-502. 2009
    ..Therefore, a further in-vivo evaluation of NLQZ-1 and NLPP-1 is worthwhile...
  12. ncbi request reprint Novel non-invasive probes for measuring tumor-hypoxia by 19F-magnetic resonance spectroscopy (19F-MRS). Studies in the SCCVII/C3H murine model
    Maria V Papadopoulou
    Evanston Northwestern Healthcare, Department of Radiation Medicine, 2650 Ridge Avenue, Evanston, IL 60201, USA
    Anticancer Res 26:3259-63. 2006
    ....
  13. ncbi request reprint Therapeutic advantage from combining paclitaxel with the hypoxia-selective cytotoxin NLCQ-1 in murine tumor- or human xenograft-bearing mice
    Maria V Papadopoulou
    The Radiation Medicine Institute, Evanston Northwestern Healthcare, 2650 Ridge Avenue, Evanston, IL 60201, USA
    Cancer Chemother Pharmacol 50:501-8. 2002
    ..The antitumor effect of paclitaxel was investigated against murine tumors and human xenografts in combination with the hypoxia-selective cytotoxin NLCQ-1...
  14. pmc Novel 3-nitro-1H-1,2,4-triazole-based compounds as potential anti-Chagasic drugs: in vivo studies
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, IL, USA
    Future Med Chem 5:1763-76. 2013
    ..Drugs currently used in the treatment of Chagas are old, partially effective and have numerous side effects...
  15. ncbi request reprint Potentiation of alkylating agents by NLCQ-1 or TPZ in vitro and in vivo
    Maria V Papadopoulou
    Department of Radiation Medicine at Evanston Northwestern Healthcare, IL 60201, USA
    J Exp Ther Oncol 5:261-72. 2006
    ..To investigate potential synergistic interactions between bioreductive agents, either NLCQ-1 or tirapazamine (TPZ) and two alkylating chemotherapeutic drugs, and how such interactions compare in vitro and in vivo...
  16. ncbi request reprint DNA repair mechanisms are involved in the hypoxia-dependent toxicity of NLCQ-1 (NSC 709257) and its synergistic interaction with alkylating agents
    Maria V Papadopoulou
    Department of Radiation Medicine, Evanston Northwestern Healthcare, Evanston, IL 60201, USA
    In Vivo 21:175-80. 2007
    ..Since NLCQ-1 targets DNA through weak intercalation, the induction of DNA lesions upon reductive metabolism may be a reasonable mechanism that predisposes cells to further damage by a subsequent alkylating agent...
  17. ncbi request reprint NLCQ-1 (NSC 709257) in combination with radiation against human glioma U251 xenografts
    Maria V Papadopoulou
    Evanston Northwestern Healthcare, Department of Radiation Medicine, Evanston, IL 60201, USA
    Anticancer Res 25:1865-9. 2005
    ..Two "advanced stage" experiments were performed in female athymic nude mice...
  18. ncbi request reprint Enhancement of the antitumor effect of cyclophosphamide with the hypoxia-selective cytotoxin NLCQ-1 against murine tumors and human xenografts
    Maria V Papadopoulou
    Radiation Medicine Institute, Evanston Northwestern Healthcare, Evanston, IL 60201, USA
    J Exp Ther Oncol 2:298-305. 2002
    ..These results suggest a potential use of NLCQ-1 in the clinic as an adjuvant to chemotherapy with CPM...
  19. ncbi request reprint NLCQ-1 (NSC 709257): exploiting hypoxia with a weak DNA-intercalating bioreductive drug
    Maria V Papadopoulou
    The Department of Radiation Medicine at Evanston Northwestern Healthcare, Evanston, Illinois 60201, USA
    Clin Cancer Res 9:5714-20. 2003
    ..Because of these results and the fact that NLCQ-1 compares favorably with the frontrunner, bioreductive compound tirapazamine, NLCQ-1 is about to enter a Phase I clinical trial...
  20. ncbi request reprint Advantage of combining NLCQ-1 (NSC 709257) with radiation in treatment of human head and neck xenografts
    Maria V Papadopoulou
    Department of Radiation Medicine, Evanston Northwestern Healthcare, Evanston, Illinois 60201, USA
    Radiat Res 168:65-71. 2007
    ..These results suggest a significant advantage in combining radiation with NLCQ-1 in treatment of human head and neck tumors, which are known to have hypoxic areas...
  21. ncbi request reprint Novel fluorinated hypoxia-targeted compounds as Non-invasive probes for measuring tumor-hypoxia by 19F-magnetic resonance spectroscopy (19F-MRS)
    Maria V Papadopoulou
    Evanston Northwestern Healthcare, Department of Radiation Medicine Evanston, IL 60201, USA
    Anticancer Res 26:3253-8. 2006
    ..19F-labeled 2-nitroimidazoles bound to hypoxic cells in tumors are known to be useful probes for measuring hypoxia, since they can allow their non-invasive detection to be carried out by 19F nuclear magnetic resonance...
  22. ncbi request reprint Mechanisms involved in the potentiation of paclitaxel or 5-fU by the hypoxic cytotoxin NLCQ-1 (NSC 709257) in vitro
    Maria V Papadopoulou
    Evanston Northwestern Healthcare, Department of Radiation Medicine, Evanston, IL 60201, USA
    Anticancer Res 25:2161-70. 2005
    ..In the present study, we investigated if the same schedule-dependent synergism seen in vivo exists in vitro as well, between NLCQ-1 and paclitaxel or 5-fluorouracil (5FU), and some of the mechanisms involved in such interactions...
  23. ncbi request reprint Synergistic enhancement of the antitumor effect of taxol by the bioreductive compound NLCQ-1, in vivo: comparison with tirapazamine
    Maria V Papadopoulou
    The Radiation Medicine Institute at Evanston Northwestern Healthcare, IL 60201, USA
    Oncol Res 13:47-54. 2002
    ..2 was obtained by TPZ in both type of tumors. These results suggest a potential clinical use of NLCQ-1 as a potentiator of taxol againstsolid tumors possessing hypoxic regions...
  24. ncbi request reprint Synthesis of novel 2-nitroimidazole-tethered tricyclic quinolines, bearing a second heteroatom, and their in vitro evaluation as hypoxia-selective cytotoxins and radiosensitizers
    Maria V Papadopoulou
    Evanston Northwestern Healthcare, Deptartment of Radiation Medicine, Evanston, IL 60201, USA
    Bioorg Med Chem Lett 14:1523-5. 2004
    ..6) values of 40.0+/-0.8 and 59.0+/-0.4 microM for 8a and 8b, respectively) but neither of the compounds was superior to 2 which does not carry a second heteroatom in the DNA-intercalating chromophore...
  25. pmc Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, Illinois 60201, United States
    J Med Chem 58:1307-19. 2015
    ..In the present work, the synthesis and in vitro and in vivo evaluation of such compounds is discussed. ..
  26. ncbi request reprint Reductive metabolism of the nitroimidazole-based hypoxia-selective cytotoxin NLCQ-1 (NSC 709257)
    Maria V Papadopoulou
    Department of Radiation Medicine at Evanston Northwestern Healthcare, 2650 Ridge Avenue, Evanston, IL 60201, USA
    Oncol Res 14:21-9. 2003
    ....
  27. ncbi request reprint NLNQ-1, a 2-[3-(2-nitro-1-imidazolyl) propylamino]-3-chloro-1,4-naphthoquinone, as a hypoxia-selective cytotoxin and radiosensitizer
    Maria V Papadopoulou
    Evanston Northwestern Healthcare, Department of Radiation Medicine, IL 60201, USA
    In Vivo 22:285-8. 2008
    ....
  28. pmc Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, IL, USA Electronic address
    Eur J Med Chem 117:179-86. 2016
    ..cruzi in structurally related subgroups of compounds. Three compounds were more potent as antichagasic agents than benznidazole but were not activated by the type I nitrorectusase (NTR). ..
  29. ncbi request reprint NLCQ-1 and NLCQ-2, two new agents with activity against dormant Mycobacterium tuberculosis
    Maria V Papadopoulou
    Department of Radiation Medicine, Evanston Northwestern Healthcare, Evanston, 2650 Ridge Ave, IL 60201, USA
    Int J Antimicrob Agents 29:724-7. 2007
    ..3, >65.3-130.6 and >50-100 for NLCQ-1, NLCQ-2 and PA-824, respectively. These results suggest the potential usefulness of these compounds in the therapy of the latent form of tuberculosis...
  30. pmc Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity
    Maria V Papadopoulou
    NorthShore University Healthsystem, Evanston, IL, United States Electronic address
    Eur J Med Chem 123:895-904. 2016
    ..Type I nitroreductase, an enzyme absent from the human host, played a role in the activation of the new compounds, which may function as prodrugs. Antichagasic activity in vivo was also demonstrated with representative propanamides. ..
  31. ncbi request reprint Synthesis of a novel nitroimidazole-spermidine derivative as a tumor-targeted hypoxia-selective cytotoxin
    Maria V Papadopoulou
    Evanston Northwestern Healthcare, Department of Radiation Medicine, Evanston, IL 60201, USA
    Bioorg Med Chem Lett 14:1519-22. 2004
    ..2-fold more sensitive to 4 under hypoxic conditions, compared to untreated cells. Similarly, radiosensitization of hypoxic V79 cells by 4 is improved in DFMO-pretreated cells...