Nitrosoureas

Johnston, Thomas P.

doi:10.1007/978-94-009-0397-5_4

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1997

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Cited by 2 publications

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“…Thus, a number of reviews − were devoted to a collection of many aspects of the chemistry and biology of N -nitrosoureas. More restricted reviews appeared on special topics such as synthesis and structure−activity relationships, − antitumor activities, − metabolism and pharmacology, − toxicology, , mutagenicity and carcinogenicity ,,− and clinical oncology. , …”

Section: Introductionmentioning

confidence: 99%

A Critical Appraisal of the Evolution ofN-Nitrosoureas as Anticancer Drugs

1997

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Section: Introductionmentioning

confidence: 99%

A Critical Appraisal of the Evolution ofN-Nitrosoureas as Anticancer Drugs

1997

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New Method to Measure the Carbamoylating Activity of Nitrosoureas by Electron Paramagnetic Resonance Spectroscopy

Gadzheva¹,

Ichimori²,

Raikov³

et al. 1997

Free Radical Research

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A new method for measuring the carbamoylating activity of nitrosoureas and isocyanates using electron paramagnetic resonance (EPR) spectroscopy is described. The extent and time course of carbamoylation reaction of chloroethyl isocyanate and a series of 9 nitrosoureas toward amino group of 4-amino-2,2,6,6-tetramethyl-piperidine-1-oxyl were examined with both the EPR method and the HPLC method which has been proposed by Brubaker et al. [Biochem. Pharmacol. 35:2359 (1986)]. Spin-labeled nitrosoureas we synthesized are included in this study since they have less toxicity or more efficiency than commercially available drug in some cases. The concentration of carbamoylated product was easily determined with the EPR spectra. There is a very high correlation (r = 0.982, t = 2.58, N = 10, p < 0.001) between the EPR and HPLC methods. Spin-labeled nitrosoureas showed lower carbamoylating activity than non-labeled analogues. The carbamoylating activity for these nitrosourea depended on the reactivity of isocyanate intermediate and almost independent of their half life. This rapid and simple EPR method is suitable for the detailed investigation of the rate and extent of carbamoylation reaction.

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Nitrosoureas

Cited by 2 publications

References 74 publications

A Critical Appraisal of the Evolution ofN-Nitrosoureas as Anticancer Drugs

A Critical Appraisal of the Evolution ofN-Nitrosoureas as Anticancer Drugs

New Method to Measure the Carbamoylating Activity of Nitrosoureas by Electron Paramagnetic Resonance Spectroscopy

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