• Bulletin of the Korean Chemical Society
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• v.32 no.10
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• pp.3634-3640
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• 2011

We have performed quantum mechanical calculations to study the geometries and binding energies of biologically important, cyclic hydrogen-bonded complexes, such as formic acid + $H_2O$, formamidine + $H_2O$, formamide + $H_2O$, formic acid dimer, formamidine dimer, formamide dimer, formic acid + formamide, formic acid + formamidine, formamide + formamidine, and barrier heights for the double proton transfer in these complexes. Various ab initio, density functional theory, multilevel methods have been used. Geometries and energies depend very much on the level of theory. In particular, the transition state symmetry of the proton transfer in formamidine dimer varies greatly depending on the level of theory, so very high level of theory must be used to get any reasonable results.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.9
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• pp.4223-4231
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• 2016

Background: Development of new apoptosis-inducing drugs is a promising trend in anticancer therapy. For this purpose several formamidinoderivatives of doxorubicin were synthesized. The aim of our study was to investigate effects of the five formamidinodoxorubicins in the ES-2 human ovarian clear cell carcinoma line, for comparison with data obtained previously for SKOV-3 human ovarian adenocarcinoma cells, to answer the question of whether and to what extent the histological cell type is a possible determinant of sensitivity to tested anthracyclines. Materials and Methods: In our experimental work the following methods were used: spectrophotometric assays with MTT; fluorimetric assays - double staining with Hoechst 33258 and propidium iodide (PI), measurement of caspase-3, -8, -9 activity, intracellular accumulation of DOX and analogues, estimation of drug uptake, mitochondrial transmembrane potential; flow cytometry - phosphatidylserine (PS) externalization with annexin V-FITC and PI fluorochromes. Results: Effects of the derivatives of doxorubicin were partially linked with the specific type of cancer cell although intracellular accumulation and cellular uptake of DOX and derivatives were similar in both. All of the investigated derivatives were considerably more cytotoxic than DOX. Formamidinodoxorubicins were able to induce caspase-dependent apoptotic cell death in both cell types. Conclusions: All new formamidine derivatives of DOX were able to induce caspase - dependent apoptosis in human ovarian cancer cell lines SKOV-3 and ES-2. Obtained results suggested that formamidine derivatives of DOX may be promising candidates for the prospective chemotherapeutic agents for the two different histological subtypes of ovarian cancer.

• Bulletin of the Korean Chemical Society
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• v.24 no.12
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• pp.1723-1724
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• 2003

• Proceedings of the Korea Technical Association of the Pulp and Paper Industry Conference
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• 2006.06b
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• pp.381-386
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• 2006

Many different types of bleaching chemicals and processes have been globally used for deinked pulp. Besides chlorine-free bleaching chemicals, hydrogen peroxide, and sodium dithionite that could be used without restriction for almost all types of fibers, chlorine-containing chemicals such as chlorine dioxide and sodium hypochlorite have also used throughout the world. Even though hydrogen peroxide is commonly used in newsprint, it could not effectively increase brightness. Experimental evaluation on the possibility of using formamidine sulfinic acid (FAS), a reducing agent, for bleaching a wood-containing deinked pulp has been carried out in this study. The effect of bleaching efficiency for FAS on operational conditions and chemical concentrations compaired to hydrogen peroxide in one and two stages was studied. FAS bleaching showed higher brightness at high temperature and low consistency, and vice versa for peroxide one. Bleaching with sodium silicate and DTPA in FAS and peroxide stage showed better results than cases without them. Sodium silicate and chelant seemed minimize the influence of transition metal ions, including manganese and iron ions, which induce both bleaching agents to decompose. As a result, FAS as a reducing agent seems more effective than hydrogen peroxide for increasing brightness and reducing yellowness. FAS and FAS sequence seemed more efficient than the other two stages of bleaching sequences with regard to the best brightness level obtained. When bleaching was conducted with FAS, COD load was just about one-third compared to peroxide, and brightness stability of the bleached pulp appeared better than peroxide after UV light irradiation.

• Journal of the Korean Chemical Society
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• v.37 no.1
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• pp.131-135
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• 1993

A new series of 2-desamino, 2-desamino-2-methyl, and 2-amino analogues of aminopterin intermediates (7a), (7b), and (7c) were synthesized from 2-amino-3-cyano-6-chloromethylpyrazine. These derivatives were synthesized via two step sequence. Thus, cyclization of 2-amino-3-cyano-6-[(S-p-carbenzyloxyphenyl)thiomethyl]-pyrazine(14) with formamidine HCl, acetamidine HCl or guanidine HCl provided condensed compounds (15a), (15b) which upon base hydrolysis yielded the desired products (7a), (7b) and (7c).

• Journal of The Korean Society of Clinical Toxicology
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• v.5 no.2
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• pp.123-125
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• 2007

Amitraz is a formamidine-derived insecticide and acaricide which is commonly used throughout the world. Amitraz intoxication is mediated through ${\alpha}_2$ adrenergic receptor agonist effects, similar to those of the ${\alpha}_2$ agonist clonidine. We report a case of a patient who experienced coma and hypotension after amitraz ingestion. A 37-year-old woman visited the ER with symptoms of vomiting and altered mental state. She had ingested a mouthful of liquid amitraz concentrate (12.5%), which rapidly led to vomiting, hypotension, bradycardia, hyperglycemia, and mental stupor. Supportive treatment, including mechanical ventilation and administration of inotropics, resulted in full recovery within four days.

• Archives of Pharmacal Research
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• v.18 no.1
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• pp.1-7
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• 1995

IY-80843, N[2-(2-methoxyphenyl)ethyl]-N'-[4-(lmidazole-4-yl)phenyl] formamidine, is a new potent $H_2-receptor$ anagonist. The potential secondary pharmacologic effects of this agent, on the central nervous and cardiovascular systems were studied. IY-80843 caused ptosis, suppression of locomotion, hypotehrmia, prolongation of sleeping time and hypotensive effects in mice, rats and dogs. These results suggest that IY-80843 affects the funcition of the central nervous and cardiovascular systems in a dose-dependent manner.

• Bulletin of the Korean Chemical Society
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• v.32 no.3
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• pp.909-914
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• 2011

An improved convergent and economical method has been developed for the synthesis of erlotinib, a 4-anilinoquinazoline and an EGFR-tyrosine kinase inhibitor for treatment of non-small-cell lung cancer. The final two steps for the formation of this 4-anilinoquinazoline from suitable 2-aminobenzonitrile intermediate and 3-ethynylaniline were modified and were performed in a simple one-pot reaction. The ring-closing mechanism for the formation of erlotinib from the suitable formamidine intermediate and 3-ethynylaniline was investigated and determined to proceed via the formation of phenyl benzamidine intermediate rather than involving Dimroth rearrangement reported earlier. The new benzamidine intermediate was isolated for the first time and characterized.

• Bulletin of the Korean Chemical Society
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• v.11 no.5
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• pp.383-386
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• 1990

We have synthesized several bicyclic heteroaromatic compounds with bridgehead nitrogen from N-amine salts of heteroaromatic amines. 2-Amino and 2-unsubstituted thiazolo[3,2-b][l,2,4]triazole derivatives 2a-b were prepared by the cyclization reaction from N-amine salts of aminothiazole-5-yl(N-methoxyimino)acetate with cyanogen bromide and formamidine acetic acid salt, respectively. 2-Methylthiazolo[3,2-b][1,2,4]triazole 2c was obtained from N-acetylated N-amine salt of aminothiazole-5-yl(N-methoxyimino)acetate by the cyclization reaction in the presence of polyphosphoric acid (PPA). 2-Substituted and 2-unsubstituted thiazole[3,2-b][1,2,4]triazole derivatives 2a-c were coupled with 7-aminocephalosporanic acid (7-ACA). Coupled cephalosporin derivatives 1a-c did not have good antibacterial activities in vitro.

• Journal of Korea Technical Association of The Pulp and Paper Industry
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• v.44 no.4
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• pp.8-15
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• 2012

Optical property improvements for ONP (old newspaper) and OMG (old magazine) were attempted by application of in-situ $CaCO_3$ formation process on recycled fiber surfaces. Washing treatment of ONP and OMG resulted in 35~40% yield loss for around 6% brightness improvement. Washing plus bleaching process with $H_2O_2$ and FAS (formamidine sulfinic acid) improved brightness and ERIC values a little more with the same amount of yield loss as washing treatment. In-situ $CaCO_3$ formation method improved those optical properties much better than the washing plus bleaching method without loss of yield, and better than the case of adding high brightness PCC up to the same ash level. It can be said that the in-situ $CaCO_3$ formation method may be used as an effective alternative for upgrading optical properties of recycled fibers.