Showing papers in "Journal of Advances in Chemistry in 2008"

Fourth Atom-Bond Connectivity Index of an Infinite Class of Nanostar Dendrimer D3[n]

Abstract: The atom-bond connectivity (ABC) index of a graph G is a connectivity topological index was defined as where d v denotes the degree of vertex v of G . In 2010, M. Ghorbani et. al . introduced a new version of atom-bond connectivity index as where In this paper, we compute a cloused formula of ABC4 index of an infinite class of Nanostar Dendrimer D 3 [n] . A Dendrimer is an artificially manufactured or synthesized molecule built up from branched units called monomers.

Calcium, Zinc and Phytate Interrelationships in Four Lesser-Known African Seeds Processed into Food Condiments

Abstract: The calcium (Ca), zinc (Zn) and phytate contents of raw, boiled, and boiled plus 72 h fermented samples of four lesser-known African seeds – Citrullus colocynthis, Cucumeropsis edulis, Ricinus communis and Prosopis africana – locally used for production of condiments in Nigeria were evaluated Zinc bioavailability of the samples were also estimated using molar ratios per kg dry weight of [phytate]:[Zn], [Ca]:[phytate] and [phytate][Ca]:[Zn] The levels of phytate, Zn and Ca of the raw seed samples varied from 15001 ± 1100 mg/100g ( C colocynthis ) to 17010 ± 1001 mg/100g ( C edulis ), 122 ± 010 mg/100g ( C colocynthis ) to 479 ± 014 mg/100g ( R communis ), and 2833 ± 258 mg/100g ( C colocynthis ) to 9824 ± 1519 mg/100g ( R communis ) respectively The calculated values of [phytate]:[Zn], [Ca]:[phytate] and [phytate][Ca]:[Zn] molar ratios for the raw seeds indicated that the samples have low Zn bioavailability However, a combined processing technique of boiling and fermentation together, unlike boiling alone, significantly (p<005) improved these molar ratio markers, indicating high Zn bioavailability in condiments produced from these seeds The implications of these findings with regards to management of Zn deficiency and the superabundance of these seeds are enormous

Study the Nature and the Effects of the Impurities of Phosphate Rock in the Plants of Production of Phosphoric Acid

Abstract: Phosphate rocks from different deposits vary widely in composition, and these variations have important effects in phosphoric acid production All phosphate rocks contain many impurities Knowledge of the nature and contents of the various elements in the phosphate is required in the manufacturing process of phosphoric acid All these chemical characteristics can help the operator to foresee its objectives under the operating conditions and the cost of production in the manufacturing process of phosphoric acid Two Tunisian natural phosphates coming from two different deposits were selected We propose in this work studying the effects of the impurities that depending on their concentration can affect decisively the behavior of these ores in the process of production of phosphoric acid Study the chemical composition of these ores is carried out according to standard analytical methods used for raw phosphates The results obtained show a slight difference in chemical properties between the two types of sedimentary phosphates and their aptitude to be used in the plants of production of phosphoric acid

Development of Simple Green Spectrophotometric and Conductometric Methods for Determination of Cephalosporins in Pure, Pharmaceutical Dosage forms and Human Urine

Abstract: Five Simple, accurate and rapid spectrophotometric and conductometric methods were developed for the determination of four third generation cephalosporins, namely, cefotaxime sodium (I) , cefoperazone sodium (II), ceftazidime pentahydrate (III) and cefdinir (IV) in pure active ingredient, pharmaceutical dosage forms and human urine. Method A: is based on the reaction of the sulphide ions produced from the alkaline hydrolysis of the cited four drugs with P- aminophenol (PAP). This reaction results in a thionine dye (phenothiazine derivative) formation which exhibits maximum absorbance at 545 nm. Method B: is based on oxidation of drug (I and III) with a known excess of n-bromosuccinimide (NBS) in acidic medium followed by the determination of unreacted amount of n-bromosuccinimide with metol and sulphanilic acid. The purple-red reaction product exhibits maximum absorbance at 520 nm. Method C: is based on the formation of yellow chelate between drug (IV) and palladium (II) chloride in buffered medium (pH 3.5) with an absorption maximum at 314 nm. Method D: is based on the reaction of drug (IV) with aqueous ninhydrin to give yellow colored product in the presence of bicarbonate with an absorption maximum at 433 nm . Method E: A conductometric method is based on the reaction of the four cited drugs with phosphotungstic acid (PTA) forming an ion associate in aqueous medium. Validation of the proposed methods was carried out. All proposed methods were successfully applied for the commercial dosage forms of the cited drugs. Method C was successfully applied for the determination of cefdinir in human urine.

Concise and Efficient Total Syntheses of Virenamides A and D

Abstract: Concise total syntheses of linear thiazole-containing peptides virenamides A ( 1 ) and D ( 4 ), isolated from Australian ascidian Diplosoma virens have been accomplished from Boc-L-valine ( 6 ) in 7 steps. A cyclization between thioamide and bromoacetaldehyde was applied to form thiazole ring as a key step.

A Nuclear Spin Selective Control over the DNA Repair Key Enzyme Might Renovate the Cancer–Fight Paradigm. DNA Polymerase Beta to Engage with a Magnetic Isotope Effect

Abstract: DNA Polymerase Beta (EC 2.7.7.7) is found to be operated by magnetic isotope effect (MIE) of Calcium once the Mg 2+ ions replaced with the stable 43 Ca 2+ isotopes inside the enzyme catalytic sites. The isotope mentioned is the only paramagnetic species of the Calcium isotopic set with a 0.135 natural abundance value and the negative 7/2 nuclear spin providing a nuclear magnetic moment equal to 1.317 Bohr magnetons. As compared to the Mg/ 40 Ca substitution, a 2.25-fold enzyme inhibition has been shown to provethe 43 Ca-MIE dependent mode of the catalysis turning down.An ion-radical mechanism based on the singlet – triplet conversion of the enzyme generated intermediates (ion-radical pairs) is found to be engaged once the paramagnetic metal isotope involved into the catalysis studied.The MIE promotes a primary reaction in DNA synthesis constituting in electron transfer between the ion – radical forming partners, [Ca(H 2 O) n 2+ ] and [Ca 2+ (dNTP)]. Once the metal isotope substitution takes place inside just one of two DNA Polymerase Beta catalytic sites, a consequent 43 Ca – promoted inhibition leads to a residual synthesis of shorted DNA fragments that counts 25 – 35 nucleotides in length contrasting with the 180 n – 210 n DNA produced by either intact or 40 Ca – loaded polymerase. Being occurred simultaneously with a marked MIE – promoted enzyme inhibition, this fact itself makes possible to consider these short (“size-invalid”) DNA segments hardly efficient in the DNA base – excision repair. The latter is a survival factor in leukemic cells where the DNApolβ was found overexpressed. That supports a standpoint considering theDNApolβ a legitimate target for antitumor agents since its inhibition deprives the malignant cell from a DNA base – excision repair in neoplasma. A possible trend making role of these data in the current developments on a novel concept - establishing chemical background for cancer therapies is in a focus.

Evaluation of IR Spectral Analysis and Dyeing Parameters for Plasma and /or Nano-Silver Treatments of Polyester and Nylon Fabrics

Abstract: In our work of this paper, we study the effect of surface modification of polyester and nylon fabrics induced by DC plasma discharge and/ or nano-siliver treatments DC plasma discharge was employed at first, as a function of plasma device parameters including different time, different current and different hydrostatic pressure using chemically inert working gas: argon or nitrogen Optimization of the performance of the applied DC plasma discharge with various applied conditions were performed using Fourier Transform Infra-Red (FTIR) Spectroscopy spectral analysis, by following up the changes in the peak intensity values of the characteristic functional groups that characterize polyester fabric Then the dyeing properties of different pretreated fabrics with plasma by the best conditions are subjected to nano-silver treatment by concentration 50 ppm under the effect of different dye concentrations, different dyeing temperature and different dyeing time Finally, the fastness properties to light and washing for the treated samples were studied The results obtained showed that both of the dyeing parameters and fastness properties were highly improved by the treatment of fabrics by either individual plasma treatment or combined DC cold plasma and nano-silver treatments

Method development and validation of simultaneous determination of seventeen metals in water by ICP/MS

Abstract: A simple, precise, accurate, and sensitive method is developed and validated for simultaneous determination of seventeen metals (Li, Sr, Ba, Tl, Pb, Bi, Al, K, Cr, Mn, Co, Ni, Cu, Zn, Mo, Ag, and Cd) in water by ICP-MS. The optimum conditions of the ICP-MS are as follows: nebulizer gas (argon) flow rate: 0.9 L/min, auxiliary gas (argon) flow 0.3 L/min, plasma (argon) gas flow: 15 L/min, reaction gas flow (helium) 4mL/min. This method is validated according to the requirements for new methods, which include linearity and range, accuracy, precision, selectivity, limit of detection (LOD), and limit of quntitation (LOQ). The current method demonstrates good linearity over the range of 1-1000 ppb with r 2 greater than 0.999 for the seventeen metals. The recovery of the metals from water samples ranges from 97.5 to 101.7%. The method is selective where minimal interferences between the metals is observed (CeO/Ce = 1%, and Ce +2 /Ce +1 = 1%), and with good resolution (0.8 amu at 10% height). The method is also precise where the RSD of the responses (cps) of replicates of the metals at three concentration levels is less than 1%. Low LOD and LOQ of metals using this method enable the detection and quantitation of these metals at low concentrations. Real water samples from West Bank in Palestine (groundwater) were analyzed for their trace metals content using this method.

Chemical and Biological Leaching Methods to Remove Heavy Metals from Sewage Sludge: A Review

Abstract: The removal of heavy metals (HMs) in sewage sludge (SS) is important since sludge is often disposed or applied on farmland to enhance soil fertility. The present study reviewed two conceptual approaches (chemical and biological leaching) of removing HMs present in SS. In the chemical leaching method, traditional acid treatment together with novel methods such as aeration, complexation and sequential extraction procedure have been reviewed extensively. Certain factors influence the removal of HMs in SS. These factors include; pH, leaching agent, redox potential, and contact time. Nitric acid (HNO 3 ), hydrochloric acid (HCl), sulphuric acid (H 2 SO 4 ), phosphoric acid (H 3 PO 4 ), ethylenediamine tetraacetic acid (EDTA), as well as Thiobacillus thiooxidans and Thiobacillus ferrooxidans are the most widely studied leaching agents and substrates involved in the chemical and bioleaching processes. However, the bioleaching process has been proposed as a safe, efficient, economical, environmental friendly method to remove HMs in SS due to its simplicity, high yield of metal extraction, low acid consumption, and low sludge solids concentration. Nevertheless, the present review has noted that most researchers are of the opinion that more studies are needed in the bioleaching method in order to enhance its commercial attraction.

Synthesis and Antimicrobial Activity of some Novel Isoindoline-1,3-Dione Derivatives

Abstract: New phthalimido derivatives incorporated with chalcone, pyrazole, pyrazoline, and pyrimidine moieties were synthesized and evaluated for their antimicrobial activities against bacterial and fungal strains. 2-{4-[1-Acetyl-5-(4-chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl} isoindoline-1,3-dione (7) showed broad spectrum antibacterial activity against both G+ and G- bacteria. While, (E)-2-{4-[3-(4-chlorophenyl)acryloyl]phenyl}isoindoline-1,3-dione (4b) showed promising antifungal activity.

New Cyanoacetamide Derivatives as Corrosion Inhibitors for Carbon Steel in Acidic Media

Abstract: The corrosion behavior of carbon steel in 1 M HCl solution in the absence and presence of 4-(2-Cyano-7- hydroxy-4-methylene-hepta-2,5-dienoylamino)-benzoic acid (a), 4-[2-Cyano-3-(4-methoxy -phenyl)-acryloylamino]-benzoicacid.(b), 4-(2-Cyano-3-phenyl acryloylamino)-benzoic acid (c) ,4-[3-(4-Chloro-phenyl)-2-cyano-acryloylamino]-benzoic acid(d), was investigated using weight loss , potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) and electrochemical frequency modulation (EFM) techniques. The inhibitive action of the investigated compounds was discussed in terms of blocking the electrode surface by adsorption of the molecules through the active centers contained in their structures. The adsorption of these derivatives on carbon steel surface is consistent with Freundlich adsorption isotherm. The effect of temperature on the rate of corrosion in the absence and presence of these compounds were also studied. Physical adsorption mechanism is proposed from the calculated thermodynamic parameters for all investigated compounds.

Corrosion Inhibition of Zinc Using Some Phenylthiazole Derivatives in Hydrochloric acid Solutions

Abstract: The inhibitive action of some phenylthiazole derivatives namely: 2-acetylamino-5-p-bromophenylazo-4-phenylthiazole (BPT), 2-acetylamino-5-p-methylphenylazo-4-phenylthiazole (MPT), 2-acetylamino-5-p-methoxyphenylazo-4phenylthiazole (XPT) and 2-acetylamino-5-p-nitrophenylazo-4-phenylthiazole (NPT), on zinc corrosion in 0.2 M HCl has been studied using weight loss, potentiodynamic polarization, electrochemical impedance spectroscopy (EIS)and electrochemical frequency modulation (EFM) measurements. The results showed that the dissolution rate of zinc decreases with increasing the phenylthiazole derivatives concentration and decreases with raising temperature. Polarization curves indicated that the studied inhibitors act as mixed-type inhibitors. The adsorption of the investigated compounds follows Langmuir adsorption isotherm model. The thermodynamic parameters of adsorption and corrosion processes were determined and discussed.

Effect of Aqueous Extract of Vitis Vinifera l. Leaf on the Rabbit Females Have Highly Thyroxine Induced by Levothyroxine Sodium

Abstract: L-Thyroxine(T4) and triiodothyronine(T3)are iodine-containing hormones produced from thyroglobulin in the thyroid follicular cells. The stimulation of metabolic rate and regulation of growth and development by these hormones appear to be due to their effects on DNA transcription and, thus, protein synthesis. The aqueous extract of vitis vinifera L. was investigated for its effect on hormones in rabbits. The aqueous extract of plant at a dose level of 50μg/rabbit showed highly significant (p<0.05)on levels of hormones T4, TSH but TSH no significant. L-thyroxine sodium treated group showed a highlysignificant increase in T3 and T4 while there was a highly significant decrease in TSH. From the above results, it is concluded for the first time that aqueous vitvs vinifera L. extract offers significant effect of T3, T4 and TSH in this rabbit females compared with control.

Colorimetric Method for Determination of some 1,4-Dihydropyridine Drugs in their Tablets and Capsules

Abstract: A simple, accurate and selective colorimetric method was developed and validated for determination of five 1,4-dihydropyridine drugs (1,4-DHP) using Tetrabutylammonium hydroxide reagent (TBAH). The proposed method was based on addition of TBAH to the studied drugs then produced yellow colors were measured spectrophotometrically. Different variables affecting the reactions conditions carefully studied and optimized and under the optimum conditions, Beer's law was obeyed in the concentration range of 2.50-40.0 µg/mL and the limits of detection were ranged from 0.750-1.956 µg/mL. The proposed method was successfully extended to pharmaceutical preparations tablets or capsules and the results which obtained were comparable with that obtained by the reference methods.

Static and Dynamic Studies of Gasoline in View of its Octane Number and its Toxic Effect

Abstract: Gasoline come primarily from petroleum cuts, it is the preferred liquid fuel in our lives. Two gasoline samples of octane numbers 91 and 95 from Saudi Arabia petrol stations were studied. This study was achieved at three different temperatures 20oC, 30oC and 50oC representing the change in temperatures of the different seasons of the year. Both the evaporated gases of light aromatic hydrocarbons (BTEX) of gasoline samples inside the tank were subjected to analyze qualitatively and quantitatively via capillary gas chromatography. The detailed hydrocarbon composition and the octane number of the studied gasoline samples were determined using detailed hydrocarbon analyzer. The idea of research is indicating the impact of light aromatic compounds in gasoline on the toxic effect of human and environment on the one hand, and on octane number of gasoline on the other hand. Although the value of octane number will be reduced but this will have a positive impact on the environment as a way to produce clean fuel.

What Is The New and Sensitive Tumor Marker for Detection of Different Kidney Tumors? Modern Study to Isolation, Purification and Characterization of N-Acetyl Galactosamine Binding Lectin From Sera Of Patients With Kidney Cancer

Abstract: The present study was designed to investigate lectins in sera of patients with kidney tumors, in addition to non tumoral kidney disease patients. Fifty five patients of malignant kidney tumors were enrolled in addition to 23 patients of benign kidney tumors, and 18 patients of non tumoral kidney diseases used as control groups, in addition to 46 healthy individuals were also investigated. The age of patients and healthy individuals were 10-90 years. The measurement of total serum proteins revealed significant (p < 0.001) decrease in patients of malignant tumors when compared with those of benign, non tumoral diseases, and healthy individuals. The conditions of the hemagglutination assay of serum lectin activity were optimized. They were Tris buffer of 20 mM and pH 7.4, 60 mM CaCl2, 800 μg of defatted serum, 30 ̊C for serum samples, 60 minutes for serum samples, and human blood of group A + suspension with 1.4 optical density. The measurement of the specific hemagglutination activity of lectins demonstrated significant (p < 0.001) elevation in patients of malignant tumors when compared with those of other patients and healthy individuals. Lectin activity was pointed out to be significantly (r = 0.767 at p < 0.0005) positively correlated with stage of malignancies. The cutoff value of the specific hemagglutination activity was found to equal 6 SHU for discriminatory malignant kidney tumors. Serum lectins activity were indicated to be inhibited by galactose, mannose, lactose, and N-acetyl galactosamine. Purification of lectin from sera of patients with malignant kidney tumors by affinity chromatography with the use of silver stain revealed N-Acetyl Galactosamine Binding Lectin (GalNAcBL). The purified folds and the yield was 178 with 32.4%. The polyacrylamide gel electrophoresis (PAGE) of purified lectin demonstrated one band consisted lectin activity. The approximate molecular weight of GalNAcBL was determined and found to be 63.83. Purified lectin was characterized through the assessment of the capability to agglutinate RBCs, inhibition by EDTA, pH dependency, thermal dependent, and carbohydrate contents. GalNAcBL were observed to be calcium dependence lectins (C-type). These results suggest that the diagnosis of the specific hemagglutination activity of lectin is promising biomarker for discrimination of malignant kidney tumor patients and the purified lectin could be introduced in the field of biomarkers.

Development and Validation of Enantiomeric Purity of Montelukast by SFC Method on Amylose Based Stationary Phase

Abstract: A new Supercritical fluid liquid chromatographic (SFC) method has been developed in normal-phase conditions for the determination of enantiomeric purity of Montelukast sodium (S,E)-2-(1-((1-3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)-3-(2-(2-hydroxypropan-2-yl)phenyl)propylthio)ethyl) cyclopropyl) acetic acid (R-isomer) (Anti asthmatic drug) in bulk drugs and in dosage forms. The sample was screened on the analytical SFC to determine the best column for the separation. The screening conditions are Column: Chiralpak AS-H (250 mm x 4.6 mm, 5 μm) column using a mobile phase system containing Supercritical fluid (Co 2 ) and 2-Propanol in the ratio (85:15% v/v). The mobile-phase compositions and the differences in separation capability of the method is noted. The resolution between two enantiomers is found to be greater than 1.5. The SFC method for the separation of enantiomers of Montelukast is proved Accurate, Precise, Linear and robust. Relative standard deviation of retention times and peak areas were better than 0.2% and 0.4%, respectively, for precision.

D/L arabinitol Ratio as an Indicator of a Healthy Lifestyle. A preliminary Study

Abstract: D-arabinitol, as opposed to the L-arabinitol, is produced by fungi of the genus Candida. The increased D/L-arabinitol ratio in body fluids is a recognized biomarker of systemic fungal infection . The factors which increase the risk of candidiasis include: sugar and confectionery, sweetened sodas, alcohol, beer, coffee, black tea, red meat, refined flour products, tobacco and salt. Often, vitamin deficiencies are caused by candidiasis of the colon. The D/L ratios in urine were determined by gas chromatography with electron capture detection (GC-ECD). For 21 examined students a questionnaire survey related to their healthy lifestyle was conducted. The lower D/L ratio in the urine of students declaring regular intake of vitamin supplements and daily consumption of fruits and/or vegetables to improve their immunity against diseases was observed. The D/ L ratio may be considered a potential indicator of a healthy lifestyle, especially in the case of young people.

Determination of the Candidiasis Marker in the Urine of Autistic Children

Abstract: Introduction: Determination of the D/L-arabinitol ratio in urine appears to be a useful diagnostic test to indicate overgrowth of Candida yeast The aim of this study was to find out whether levels of D/L-arabinitol ratio in the urine of children with autism are heightenedMaterial and methods: D/L-arabinitol ratio in urine was determined by capillary gas chromatography with electron capture detection (GC-ECD) Urine samples were collected from 83 autistic children (25–16 years old) and from 50 healthy children (15-16 years old)Results: (1687%) of autistic children under study had an elevated D/L ratio in urine (>425) For 8 of them, the stated norm was exceeded less than twice (D/L: 439-698); for 4 of them the levels of D/L-arabinitol were higher than cutoff limit 2-3 times (D/L: 857-116); for 1 child the norm was exceeded over 5-times (D/L: 2176); 1 child had a highly rebounding value (D/L: 8913) Conclusion: Some of the autistic children show a raised D/L- arabinitol ratio in urine Such percentage, in comparison to that reported in literature for other hospitalized patients, is lower than in the case of hematological, cardiac diseases and cancer, but higher than in the case of children from intensive care unit and persons after long term antibiotic therapies

Colorimetric Determination of Fluoride in Drinking Groundwater using a Polymeric Zirconium Complex of 5-(2-Carboxyphenylazo)-8-Hydroxyquinoline

Abstract: A sensitive colorimetric determination of fluoride in drinking water has been developed using a polymeric zirconium complex of 5-(2-Carboxyphenylazo)-8-Hydroxyquinoline as fluoride reagents. The method allowed a reliable determination of fluoride in range of (0.0-1.5) mg L -1 . The molar absorptivity of the complex formation is 7695 ± 27 L mol -1 cm -1 at 460 nm. The sensitivity, detection limit, quantitation limit, and percentage recovery for 1.0 mg L -1 fluoride for the proposed method were found to be 0.353 ± 0.013 μg mL -1 , 0.1 mg L -1 , 0.3 mg L -1 , and 101.7 ± 4.1, respectively.

Enzymatic Synthesis of Nucleoside Triphosphates. Does It Involve An Ion-Radical Path ?

Abstract: Accumulation and release of energy in the nucleoside triphosphate enzymatic synthesis and hydrolysis does not limited to a routine energy consuming nucleophilic mechanism. These processes require an overcoming the large energy barrier exceeding a total value of accumulated or released energy level by at least 3 – 4 times (~10 kcal/mol). This energy is supposed to be taken from the mechanical compression of the catalytic site and used to form P–O chemical bond by a direct nucleophilic addition of phosphate to nucleoside diphosphate (ADP as an example). A new, energetically “cheap”, ion-radical mechanism of the ATP biosynthesis has been proposed due to the observation of magnetic isotope and magnetic field effects on the ATP synthesis. This mechanism is about to generate a compression energy to “spend” on a partial dehydratation of magnesium ion inside the nucleotidyl transferase catalyric site (energy cost of this process is 35 kcal/mol, i.e. by 23 times less than a total accumulated or released energy). Dehydration of this ion is to increase its electron affinity and hence to stimulate an electron transfer from ADP 3to Mg 2+ . This reaction is a starting point of the ionradical mechanism considering the molecular mechanics of enzymatic machines and its quantum chemistry background as well. To the contrast of a hardly controllable nucleophilic path, the ion-radical mechanism might be turned on/off by a targeted delivery of paramagnetic magnesium ions, 25 Mg 2+ , towards the phosphate transferring enzyme catalytic site. The magnesium isotope substitution is easily reachable by the endo-osmotic pressure techniques, which makes it attractive for further biotechnological and/or pharmacological application(s).

Ultrasonic Waves Assisted Synthesis of Curcuminoids Based on 3-Methylacetylacetone and in Situ Synthesis of Gold Nanoparticles Capped with Curcuminoids

Abstract: Ultrasonic irradiation was used to induce the Knuevenagle reaction between aromatic aldehydes and 3-methylacetylacetone to synthesize curcumin analogues with moderate to good yields. The structures of the compounds were established by elemental analysis and from their mass and 1 HNMR spectra. In situ curcumin-gold nanoparticles were synthesized. The solutions of the prepared nanoparticles have purple to deep-red colors and their UV-vis spectra were characterized by the Surface Plasmon Resonance bands within the range 538-554 nanometer.

Synthesis of 2, 3-Dihydro-1,4-naphthaquinone Derivatives for Targeting the Altered Cancer Cells Metabolism

Abstract: A new four derivatives of 2,3-Dihydro-1,4-naphthaquinonewere synthesizedas possible bioreductiveprodrugs for5-fluorouracil (5-Fu),Mercaptopurine (6-MP), N-acetyl cysteine (NAC)and 3-bromopyrovic acid (3-BPA) to selectively deliver the drugs into the cancer cells and these are:2-((5-fluoro-1,2-dihydropyrimidin-4-yloxy)methyl)-3-hydroxy naphthalene-1,4dione(compound A),2-((9H-purin-6-ylthio)-3-hydroxyl naphthalene-1,4dione(compound B)acetmido-3-((3-methyl-1,4-dihydronaphthalen-2-yl)methylthio)propanoicacid (compound C)and hydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)methyl3-bromo-2-oxopropanoate ( compound D)Their chemical structures were characterized by H1 NMR, IR spectroscopy and elemental microanalysisThe in vitro antitumor activity tests againstHep-2 human larynx cancer cell lineindicated that compound A,B,C and D havesignificant anticancer activities when compared with 5-Fu

Experimental and Theoretical Investigations of Complex Formation of Substituted Phenylazo-Derivatives of Methylphloroglucinol

Abstract: Using spectrophotometric titration technique, the processes of complex formation of some phenylazo-derivatives of methylphloroglucinol (MPG) containing hydroxo-, nitro- and nitroso-substituents were studied. The spectral criteria of neutral and ionized forms of the organic ligands in their different tautomeric forms were determined. It was detected that the complex formation is accompanied by formation of one or two chelate cycles which involve azo- or nitroso-fragments and neighboring OH-groups of the organic ligands. Different types of coordination lead to different changes in the electronic absorption spectra. The DFT-B3LYP modeling of a Ni(II) complex of α-hydroxyphenylazo MPG established the most probable coordination mode of the organic ligand: tridentate chelating dianion, distorted square coordination of Ni-cations including one water molecule. The theoretical results are in a good accordance with the experimental data.

Synthesis of Some New Tetracyclic Pyrimidine Derivatives Using Exocyclic α,β-Unsaturated Ketone and Evaluation of Their Antitumor Activities

Abstract: Thiazolopyrimidine 2 was obtained from the reaction of dihydropyrimidinone with chloroacetic acid and benzaldehyde. Thiazolopyrimidine 2 containing an α,β-unsaturated ketonic function [-CH=CH-CO-] has been used as a component of Michael addition with an equimolar amount of dinucleophiles to give a series of novel tetracyclic pyrimidine derivatives. Treatment of thiazolopyrimidine 2 with uracil, aminotriazole, cyanoacetic acid hydrazide, o-phenylenediamine or diaminopyridine afforded the corresponding pyridopyrimidine, triazolopyrimidine, pyrazolone, benzodiazepine and triazepine derivative, respectively. The detailed synthesis, spectroscopic data, and antitumor activity for synthesized compounds were reported.