Method of Assay for Ethylenimine Derivatives

Allen, Eugene M.; Seaman, William

doi:10.1021/ac60100a014

Cited by 50 publications

(10 citation statements)

References 22 publications

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“…of 275). This agrees with the result obtained by this method for trzs(2,2-di-methyl-l-aziridiny1)phosphine oxide (18) 82.5-82.9'/747 mm.] , was separated by fractional distillation through a spinning band column.…”

supporting

confidence: 90%

Synthesis of Potential Dual Antagonists III

Bardos

Barua

Chmielewicz

et al. 1965

Journal of Pharmaceutical Sciences

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supporting

confidence: 90%

Synthesis of Potential Dual Antagonists III

Bardos

Barua

Chmielewicz

et al. 1965

Journal of Pharmaceutical Sciences

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“…The reaction of aziridines ( R = H , triazinyl) with thiosulfate yields S-alkyl thiosulfates (131,132), which are known as Bunte salts (133).…”

Section: Reaction With Nitrogenmentioning

confidence: 99%

Imines, Cyclic

Scherr¹,

Steuerle²,

Fikentscher³

2000

Kirk-Othmer Encyclopedia of Chemical Technology

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“…The compounds were dissolved in C0,-free deionized water (1.2 g/lOO ml) and incubated a t 37 C. Aliquot samples (10 ml) were taken a t various time intervals and the intact aziridine rings were determined by the titrimetric method of Allen and Seaman (Bardos et al, 1965b;Allen and Seaman, 1955).…”

Section: Hydrolysis Studiesmentioning

confidence: 99%

“…Both compounds (as well as all other 2,2-dimethylaziridine derivatives) give, a t zero time, a titration value of approximately 50% of the theoretical amount, in contrast t o unsubstituted or not germinally substituted aziridines which are 100% 'titratable.' This is a characteristic inherent in the analytical method of Allen and Seaman (Bardos et al, 19653;Allen and Seaman, 1955).…”

Section: Hydrolysis Studiesmentioning

confidence: 99%

Studies on the chemistry, antitumor activity, and pharmacology of ethyl Di‐(2,2 ‐dimethyl)ethylenamido phosphate (AB‐163)

Munson

Babbitt

Chmielewicz

et al. 1969

Journal of Surgical Oncology

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AB-163, a new alkylating agent containing the 2,2-&methylaziridine moiety, was found to be active against a number of transplanted and virus-induced tumor systems in mice. This compound hydrolyzes in water a t 37 C. The hydrolysis product was isolated and identified as ethanol and amino-tert-butyl phosphate. The compound was shown to react with the model nucleophile 4-(p-nitrobenzyl) pyridine (NBP) comparably to previously studied alkylating agents. The intravenous LD,, was 198 mg/kg and the intraperitoneal LD,,, was 159 mg/kg in ICR/Ha male mice. I n mice carrying Ehrlich ascites tumor (E-2), 30 mg/kg of AB-163 resulted in 95% tumor inhibition. I n Sarcoma-180 inoculated mice, 15 mg/kg caused a 20-30% apparent cure rate and a 62% tumor inhibition of the animals having tumors. Against Adenocarcinoma 755,40 mg/kg exhibited a 60% cure rate and 50% tumor inhibition of the animals with tumors. Leukemia LIZ10 treated on days 1-11 was cured in 20-30y0 of the animals receiving 30 mg/kg of AB-163 and there was a 76-170% increase in survival time in the remaining animals. In animals infected with Friend virus, a 40 mg/kg dose resulted in 65% reduction of splenic weight as compared to controls. Studies in dogs indicated that the main toxicity is hematopoietic depression. Terminally, depression of liver functions was observed. High doses produced central nervous system effects which manifested themselves in loss of appetite, vomiting, increased salivation, lethargy, and convulsions.

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Method of Assay for Ethylenimine Derivatives

Cited by 50 publications

References 22 publications

Synthesis of Potential Dual Antagonists III

Synthesis of Potential Dual Antagonists III

Imines, Cyclic

Studies on the chemistry, antitumor activity, and pharmacology of ethyl Di‐(2,2 ‐dimethyl)ethylenamido phosphate (AB‐163)

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