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At least 973 records · Page 54Linked to original sources
PubMed1976

Synthesis and in vitro cytotoxic activity of new n-diazoacetylglycine derivatives.

The syntheses of various N-diazoacetylglycine derivatives are described. The results of an in vitro screening carried out on KB cells for cytotoxic activity are reported. The most active compounds are DGE, DGiBA and DGHA. A possible relationship between the activity and the liposolubility of these compounds is discussed.

Antineoplastic Agents↗
PubMed1976

Diamide acts intracellularly to enhance transmitter release: the differential permeation of diamide, DIP, DIP+1 and DIP+2 across the nerve terminal membrane.

The actions of the new potent thiol oxidizing agents, diazene dicarboxylic acid bis (N'-methyl piperazide) (DIP) and the N'-methyl iodide (DIP + 1) and the bis-N'-methyl iodide (DIP + 2) salts of DIP, were tested at the frog neuromuscular junction. At 20 degrees C, DIP was as fast as the thiol oxidizing agent, diamide, in evoking transmitter release but was appreciably less effective at 6 degrees C. DIP + 1 and DIP + 2 did not increase transmitter release. Since the three agents are potent oxidizers of glutathione and since the effectiveness of the compounds appears to depend on their ability to exist, at least in part, in a neutral form at physiological pH, it is concluded that their action as promoters of transmitter release depends on their ability to permeate nerve terminal membranes. Thus, both diamide and DIP act to increase transmitter release by the intracellular oxidation of glutathione. The two charged agents, DIP + 1 and DIP + 2, are potent muscular depolarizing agents. It is probable that the quaternary nitrogen groups of these compounds render them cholinomimetics.

Acetylcholine↗
PubMed2006

Photocatalytic degradation of C.I. Acid Red 27 by immobilized ZnO on glass plates in continuous-mode.

The photocatalytic degradation of C.I. Acid Red 27 (AR27), an anionic monoazo dye of acid class, in aqueous solutions was investigated with immobilized ZnO catalyst on glass plates in a continuous-mode. In the slurry ZnO system the separation and recycling of the photocatalyst is practically difficult. Thus, ZnO was immobilized on solid supports to solve this problem. The removal percent increases with increasing the photoreactor volume and light intensity but it decreases when the flow rate is increased. With decreasing flow rate from 43 to 15mlmin(-1), the complete decolorization and degradation was obtained at around 748 and 1080cm(3) from photoreactor volume. The increase in the light intensity from 21.4 to 58.5Wm(-2) increases the decolorization from 23 to 57.6% and degradation from 17.5 to 37.8% for 374cm(3) of photoreactor volume. NH(4)(+), NO(3)(-), NO(2)(-) and SO(4)(2-) ions were analyzed as mineralization products of nitrogen and sulfur heteroatoms. Results showed that final concentration of SO(4)(2-) ions and N-containing mineralization products were less than the finally expected stoichiometric values. The positive slope of production of NH(4)(+), NO(3)(-) and NO(2)(-) shows that these compounds are initial products resulting directly from the initial attack on the nitrogen-to-nitrogen double bond (-NN-) of the azo dye.

Amaranth Dye↗
PubMed1977

Antimetastatic effects of N-diazoacetyl-glycine derivatives in C57BL mice.

When three diazoacetyl-glycine derivatives, N-diazoacetyl-glycine amide (DGA), N-diazoacetyl-glycine hydrazide (DGI), and N-diazoacetyl-glycine ethyl ester (DGE), were tested against Lewis lung carcinoma in C57BL mice, DGA reduced sharply the number and weight of pulmonary metastases; the effects of DGI and DGE were less pronounced. The growth of the primary tumor was reduced slightly by DGA, but the greater effect was produced by DGI. The absence of correlation between the reduction of the growth of the primary implant and the number of lung secondary tumors for the tested compounds indicated that DGA possesses antimetastatic properties.

Animals↗
PubMed1976

Colon carcinogenesis in germ-free rats with intrarectal 1,2-dimethylhydrazine and subcutaneous azoxymethane.

The effect of intestinal microflora on colon carcinogenesis by 1,2-dimethylhydrazine and azoxymethane was studied, with the use of germ-free and conventional female Fischer rats. At 7 weeks of age, germ-free and conventional rats were treated with 20 weekly intrarectal 1,2-dimethylhydrazine (20 mg per kg body weight per week) or subcutaneous azoxymethane (10 mg per kg body weight per week) doses and were autopsied 15 weeks later. Tumors were induced in the small intestine and colon of germ-free and conventional rats treated with intrarectal 1,2-dimethylhydrazine; the number of rats with colon tumors and the multiplicity of tumors were decreased in germ-free rats, compared with conventional animals. Azoxymethane given subcutaneously increased the incidence and multiplicity of colon tumors in germ-free rats, compared with conventional controls. It is concluded that the intestinal microflora alter the carcinogenic and/or cocarcinogenic effect of different compounds in the large intestine.

Animals↗
PubMed1977

Inactivation studies of cathepsin D with diazo compounds.

Cathepsin D was inactivated with various diazo compounds at very high concentration. Reaction proceeded maximally at pH 4.5 in the presence of cupric ions. With 3-diazo-indazole and triazene the inactivation was noted also in the absence of cupric ions what indicates that the mechanism is mediated through triazene. CD-spectrum of partially inactivated enzyme shows that conformational changes occurred after treatment with diazo compound.

Animals↗