Literature DB >> 7236487

In vitro metabolism of misonidazole.

P D Josephy, B Palcic, L D Skarsgard.   

Abstract

Misonidazole (MISO) is a nitroimidazole drug currently undergoing clinical trials as a radiosensitizer of hypoxic tumour cells. The drug is also toxic to such cells, probably because of metabolic activation of the nitro group under hypoxia. The metabolic fate of 14C-labelled MISO is examined, using hypoxic mammalian (CHO) cells in vitro. Organic-soluble and acid-soluble metabolites are formed, and radioactivity is bound to macromolecules. The organic-soluble products are separated by TLC and HPLC. Evidence is presented to show that one of the metabolites is hydroxylamino-misonidazole. The significance of metabolic nitroreduction is discussed.

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Year:  1981        PMID： 7236487      PMCID： PMC2010618          DOI： 10.1038/bjc.1981.65

Source DB:  PubMed          Journal:  Br J Cancer        ISSN： 0007-0920            Impact factor:   7.640


  16 in total

1.  The mechanism of microsomal and mitochondrial nitroreductase. Electron spin resonance evidence for nitroaromatic free radical intermediates.

Authors:  R P Mason; J L Holtzman
Journal:  Biochemistry       Date:  1975-04-22       Impact factor: 3.162

2.  Electron spin resonance-spin trapping. Detection of superoxide formation during aerobic microsomal reduction of nitro-compounds.

Authors:  R C Sealy; H M Swartz; P L Olive
Journal:  Biochem Biophys Res Commun       Date:  1978-05-30       Impact factor: 3.575

3.  Radiosensitizing and toxic effects on the 2-nitroimidazole Ro-07-0582 in hypoxic mammation cells.

Authors:  B A Moore; B Palcic; L D Skarsgard
Journal:  Radiat Res       Date:  1976-09       Impact factor: 2.841

4.  Sensitizing and toxicity properties of misonidazole and its derivatives.

Authors:  G F Whitmore; S Gulyas; A J Varghese
Journal:  Br J Cancer Suppl       Date:  1978-06

Review 5.  The use of nitroaromatic compounds as hypoxic cell radiosensitizers.

Authors:  P Wardman
Journal:  Curr Top Radiat Res Q       Date:  1977-08

6.  Differences in the toxicity and metabolism of the 2-nitroimidazole misonidazole (Ro-07-0582) in HeLa and Chinese hamster ovary cells.

Authors:  Y C Taylor; A M Rauth
Journal:  Cancer Res       Date:  1978-09       Impact factor: 12.701

7.  Ascorbate-enhanced cytotoxicity of misonidazole.

Authors:  P D Josephy; B Palcic; L D Skarsgard
Journal:  Nature       Date:  1978-01-26       Impact factor: 49.962

8.  Hypoxia-dependent reduction of 1-(2-nitro-1-imidazolyl)-3-methoxy-2-propanol by Chinese hamster ovary cells and KHT tumor cells in vitro and in vivo.

Authors:  A J Varghese; S Gulyas; J K Mohindra
Journal:  Cancer Res       Date:  1976-10       Impact factor: 12.701

9.  Pharmacokinetics of hypoxic cell radiosensitizers: a review.

Authors:  P Workman
Journal:  Cancer Clin Trials       Date:  1980

10.  Pharmacokinetic and metabolic studies of the hypoxic cell radiosensitizer misonidazole.

Authors:  I R Flockhart; P Large; D Troup; S L Malcolm; T R Marten
Journal:  Xenobiotica       Date:  1978-02       Impact factor: 1.908
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  5 in total

Review 1.  Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950-2021 Comprehensive Overview.

Authors:  Ria Gupta; Sumit Sharma; Rohit Singh; Ram A Vishwakarma; Serge Mignani; Parvinder Pal Singh
Journal:  Pharmaceuticals (Basel)       Date:  2022-04-30

2.  Epigenetic modulation and apoptotic induction by a novel imidazo-benzamide derivative in human lung adenocarcinoma cells.

Authors:  Amrutha Arjunan; Sankar Pajaniradje; Arul Prakash Francis; Srividya Subramanian; Sathyapriya Chandramohan; D Parthasarathi; Ayyiliath M Sajith; M Syed Ali Padusha; P P Mathur; Rukkumani Rajagopalan
Journal:  Daru       Date:  2021-10-12       Impact factor: 4.088

3.  Distribution and tumor penetration properties of a radiosensitizer 2-[14C] misonidazole (Ro 07-0582), in mice and rats as studied by whole-body autoradiography.

Authors:  G Akel; P Benard; P Canal; G Soula
Journal:  Cancer Chemother Pharmacol       Date:  1986       Impact factor: 3.333

Review 4.  Imidazoles as potential anticancer agents.

Authors:  Imran Ali; Mohammad Nadeem Lone; Haasan Y Aboul-Enein
Journal:  Medchemcomm       Date:  2017-04-13       Impact factor: 3.597

Review 5.  The Therapeutic Potential of Imidazole or Quinone-Based Compounds as Radiosensitisers in Combination with Radiotherapy for the Treatment of Head and Neck Squamous Cell Carcinoma.

Authors:  Abul Azad; Anthony Kong
Journal:  Cancers (Basel)       Date:  2022-09-27       Impact factor: 6.575
  5 in total

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