مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

video

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

sound

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Persian Version

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

View:

314
مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Download:

125
مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Cites:

Information Journal Paper

Title

SYNTHESIS, IN VITRO AEROBIC AND HYPOXIC CYTOTOXICITY AND RADIOSENSITIZING ACTIVITY OF NOVEL METRONIDAZOLE TETHERED 5-FLUOROURACIL

Pages

  1-8

Abstract

 Background and the purpose of the study: Several 2, 4-dinitrophenyl and 2, 4-dinitrophenylamine tethered 5-FU (5-fluorouracil) compared to their components have shown minimal or no CYTOTOXICITY to HT-29 cell line under aerobic conditions but high CYTOTOXICITY and RADIOSENSITIZING effects under hypoxic conditions. In the present study the CYTOTOXICITY and radiation potentiation of three novel analogues of these compounds by replacing 2, 4-dinitrophenyl moiety with 2-methyl-5-nitroimidazole, a known radiosensitizer and cytotoxic agent was investigated.Methods: Tethered compounds 7–9 were prepared by the reaction of 1- (t-butoxycarbonyl) -5-fluorouracil 6 with METRONIDAZOLE esters 2–4 followed by removal of the t-butoxycarbonyl protecting group. CYTOTOXICITY of compounds in HT-29 cells with or without radiation were determined by 3- (4, 5-Dimethylthiazol-2-yl) -2, 5-diphenyltetrazolium bromide (MTT), propidium iodide (PI) -digitonin and clonogenic assays.Results: Tethered compounds 7-9 induced time-and concentration–dependent CYTOTOXICITY under hypoxia but had no significant effect under aerobic conditions. These compounds also showed selective and concentration- dependent radiosensitization effects under hypoxic conditions.Conclusion: Tethered compounds 7-9 compared to 5-FU 5 showed minimal cytotoxicities under aerobic and selective RADIOSENSITIZING activities under hypoxic conditions. Also effects of these compounds were higher than those of METRONIDAZOLE 1 which is a known cytotoxin and radiosensitizer under hypoxic conditions.

Cites

  • No record.

    • References

  • No record.

    • Cite

    APA: Copy

    ABDI, KHOSRO, KHALAJ, ALI, OSTAD, SEYED NASSER, LAMEI, NAVID, & KHOSHAYAND, MOHAMMAD REZA. (2013). SYNTHESIS, IN VITRO AEROBIC AND HYPOXIC CYTOTOXICITY AND RADIOSENSITIZING ACTIVITY OF NOVEL METRONIDAZOLE TETHERED 5-FLUOROURACIL. DARU JOURNAL OF PHARMACEUTICAL SCIENCE, 21(9), 1-8. SID. https://sid.ir/paper/275746/en

    Vancouver: Copy

    ABDI KHOSRO, KHALAJ ALI, OSTAD SEYED NASSER, LAMEI NAVID, KHOSHAYAND MOHAMMAD REZA. SYNTHESIS, IN VITRO AEROBIC AND HYPOXIC CYTOTOXICITY AND RADIOSENSITIZING ACTIVITY OF NOVEL METRONIDAZOLE TETHERED 5-FLUOROURACIL. DARU JOURNAL OF PHARMACEUTICAL SCIENCE[Internet]. 2013;21(9):1-8. Available from: https://sid.ir/paper/275746/en

    IEEE: Copy

    KHOSRO ABDI, ALI KHALAJ, SEYED NASSER OSTAD, NAVID LAMEI, and MOHAMMAD REZA KHOSHAYAND, “SYNTHESIS, IN VITRO AEROBIC AND HYPOXIC CYTOTOXICITY AND RADIOSENSITIZING ACTIVITY OF NOVEL METRONIDAZOLE TETHERED 5-FLUOROURACIL,” DARU JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 21, no. 9, pp. 1–8, 2013, [Online]. Available: https://sid.ir/paper/275746/en

    Related Journal Papers

  • No record.

    • Related Seminar Papers

  • No record.

    • Related Plans

  • No record.

    • Recommended Workshops






    Move to top
    telegram sharing button
    whatsapp sharing button
    linkedin sharing button
    twitter sharing button
    email sharing button
    email sharing button
    email sharing button
    sharethis sharing button