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A simple and economical method for modifying chitosan based on non-catalytic direct condensation reaction between chitosan and phenolic acids “Gallic and Caffeic acids” has been developed to produce condensation adduct resins RI and RII. The resins structure and morphology were confirmed by physical and chemical tools such as FTIR, SEM, EDX, XRD elemental analysis, TGA, water regain, dissociation in acidic medium, and point of zero charge. The new resins were evaluated as silver ions adsorbents. Factors affecting adsorption, as well as kinetics, equilibrium, and thermal properties of adsorption, were studied using conventional equations. The new resins showed more efficient removal of toxic silver ions from the aqueous medium than parent chitosan polymer. The maximum adsorption capacity amounted to 67.5, 300, and 278 mg/g with removal efficiency reaching 22.5%, 100%, and 92.66% for chitosan, RI, and RII; respectively at pH 6.5 and initial silver concentration 300 mg/L. The new resins showed spontaneous chemisorption toward silver ions with exothermic nature for RI, and endothermic nature for RII. The new condensation adduct resins showed good re-use ability reaching 83% and 67% for RI and RII; respectively, by using 0.01 M nitric acid solution.

Wild plants growing in the Egyptian deserts are facing abiotic stress, which can lead to interesting & safe natural products possessing potential chemical profiles. Consequently, our study was designed to assess the phytochemical composition of the aerial parts of Limonium tubiflorum (family Plumbaginaceae) growing wild in Egypt for the first time. In addition, in silico screening and molecular dynamic simulation of all isolated phytoconstituents were run against the main protease (M-pro) and spike glycoprotein SARS-CoV-2 targets which displayed a crucial role in the replication of this virus. Our findings showed that the phytochemical investigation of 70% ethanol extract of L. tubiflorum aerial parts afforded six known flavonoids;myricetin 3-O-(2 ''-galloyl)-beta-D-galactopyranoside (1), myricetin 3-O-(2 ''-galloyl)-alpha-L-rhamnopyranoside (2), myricetin 3-O-(3 ''-galloyl)-alpha-L-rhamnopyranoside (3), myricetin 3-O-beta-D-galactopyranoside (5), apigenin (6), myricetin (7), along with two known phenolic acid derivatives;gallic acid (4) and ethyl gallate (8). Docking studies revealed that compounds (1) & (2) were the most effective compounds with binding energies of -17.9664 & -18.6652 kcal mol(-1) against main protease and -18.9244 & -18.9272 kcal mol(-1) towards spike glycoprotein receptors, respectively. The molecular dynamics simulation experiment agreed with the docking study and reported stability of compounds (1) and (2) against the selected targets which was proved by low RMSD for the tested components. Moreover, the structure-activity relationship revealed that the presence of the galloyl moiety is necessary for enhancement of the activity. Overall, the galloyl substructure of myricetin 3-O-glycoside derivatives (1 and 2) isolated from L. tubiflorum may be a possible lead for developing COVID-19 drugs. Further, in vitro and in vivo assays are recommended to support our in silico studies.

Numerous microRNAs (miRNAs) have been observed to be abnormally expressed in cancer. Therefore, miRNA signatures could be potential noninvasive diagnostic and prognostic biomarkers for hepatocellular carcinoma (HCC).To correlate miRNA-29a and miRNA-124 expression levels with the clinical features and survival rates of HCC patients.Serum miRNA expression in 150 samples (50 patients with HCC, 50 patients with liver cirrhosis, and 50 healthy controls) were quantified using real-time qRT-PCR.The expression levels of serum miRNA-29a were higher and the levels of miRNA-124 were lower in patients with HCC than in patients with liver cirrhosis and controls. ROC curve analysis showed promising accuracy for both miRNAs in distinguishing patients with HCC from those with liver cirrhosis. Levels of miRNA-29a were related to tumor number, size, stage, and outcome, whereas levels of miRNA-124 were related to vascular invasion. The overall survival rate of patients with low miRNA-29a expression was significantly higher than that of patients with high expression. Additionally, the multivariate analysis identified miRNA-29a as an independent prognostic variable.The investigated miRNAs showed acceptable accuracy in the diagnosis of HCC; therefore, both could be utilized as diagnostic biomarkers. Additionally, miRNA-29a could be used as a prognostic biomarker.

Wild plants growing in the Egyptian deserts are facing abiotic stress, which can lead to interestingsafe natural products possessing potential chemical profiles. Consequently, our study was designed to assess the phytochemical composition of the aerial parts of

Objective To study the potential role of miRNA34a gene expression and its relationship with P53 gene expression, fate, stage, metastasis and overall survival of colorectal cancer. Patients and methods This study was carried out 30 patients with colon adenocarcinoma, 30 patients with benign colon polyp and 30 apparently healthy persons served as controls. All participants were subjected to full history taking, general clinical examination. Complete blood count, liver and kidney function, determination of serum tumor markers were done. Estimation of microRNA 34a and P53 Gene expression by real-time PCR were done. Results There was a significant negative relationship between serum tumor markers and micro RNA 34a gene expression in cancer patients. Also, there was a statistically significant positive relationship between miRNA34a gene expression and P53 gene expression in both patients groups. The diagnostic accuracy of miRNA34a gene expression was both sensitive and specific for colon cancer. MiRNA34a and P53 gene expression had statistically significant relation with tumor stage and presence of metastases. Conclusion It can be concluded that the level of miRNA34a can be used to differentiate between colon cancers and begin adenomas. MiRNA34a can be used as a prognostic marker in colon cancer., Highlights • MiRNA34a has an important role in colon cancer. • Presence of correlation between P53 and miRNA34a gene expression. • MiRNA34a can be used as a prognostic marker in colon cancer. • MiRNA34a can be used to differentiate between colon cancer and benign adenoma.

Clinical outcome of T2DM can be influenced by a polymorphism of different cytokines. The aim of this study was to evaluate the effect of genetic variation and gene expression of IL-4 in T2DM patients. This study was carried out on type II diabetic patients and healthy people served as controls. All subjects were submitted to estimation of IL-4 gene polymorphism using VNTR PCR method and gene expression by real-time PCR. There was a significant decrease of IL-4 gene expression and serum IL4 levels in subjects with B2B2 genotypes. A significant positive correlation was found between IL-4 gene expression and the HDL-c levels and negative correlation between serum IL4 levels and LDLc. Also, a negative correlation was found between serum IL4 and gene expression with both systolic and diastolic blood pressure levels in patients group. It can be concluded that IL-4 gene expression and serum IL4 reduction in patients with B2B2 genotypes has a relation to dyslipidemia and hypertension in the patient with type 2 diabetes mellitus.

Colorectal cancer (CRC) is a common cancer worldwide that affects men and women of all racial and ethnic groups. Recent evidence supports the role of microRNAs in CRC. We planned to investigate microRNA200c expression and its relation with diagnosis, prognosis, metastasis and overall survival in CRC patients. This study enrolled 90 subjects (3'0 CRC patients, 30 patients with benign colorectal polyps and 30 healthy control subjects).Laboratory investigations included measurement of serum CA19-9 and CEA by enzyme linked immunosorbent assay (ELISA) method and relative quantitation (RQ) of microRNA200c gene expression by real time PCR technique.Significant higher MicroRNA200c expression levels in CRC patients versus both benign (P 0.011) and control groups (P 0.001), additionally, benign group had elevated levels versus control (P 0.001). MicroRNA 200c at cutoff4.56 had sensitivity 86.67% and specificity 73.33% (P 0.001) for CRC discrimination. Kaplan-Meier survival analysis revealed significant association (P = 0.028) of high expression of microRNA200c with decreased overall survival.Noticeable up-regulation of microRNA200c in CRC and its remarkable relation with unfavorable survival suggesting its potential dual use as a diagnostic and prognostic biomarker for CRC.

Background and objectives Sepsis is one of the major factors for both term and preterm babies with morbidity and mortality. On the basis of recent clinical trials, altered circulating micro-RNAs (miRNAs) may serve as possible biomarkers in sepsis for diagnosis and prognosis. The aim of this research is to assess the diagnostic and prognostic biomarkers of miRNA 15b and miRNA 378a for neonatal sepsis. Subjects & methods This study was carried out 25 neonates with sepsis admitted to neonatal ICU of Menoufia University Hospital and 25 healthy controls from February 2019 to May 2020. The relative quantification (RQ) of miRNA-15b and miRNA-378a expression was assessed using real time PCR technique. Results: Our results demonstrated that patients with sepsis had significantly higher level of MiRNA-15b than the healthy volunteers. On the other hand, patients with sepsis had significantly lower level of MiRNA-378a than the healthy volunteers. The ROC curve showed that the serum MiRNA-15b was a significant discriminator of sepsis with a combined sensitivity and specificity of 76% and 88% with cutoff point of 3.24. In addition, serum MiRNA-378a was a significant discriminator of sepsis with a combined sensitivity and specificity of 60% and 88% with cutoff point of 0.361. The miRNA-15b expression significantly correlated positive with respiratory rate (r =0.415,p =0.039), WBCs (r = 0.408, p =0.043), and CRP (r =0.407, p=0.043). Likewise, miRNA-378a expression significantly correlated negative with respiratory rate (r =-0.415p =0.024), WBCs (r =- 0.442, p =0.027), and CRP (r =- 0.459, p=0.021). Conclusion Both MiRNA 15b and 378a are promising biomarker for neonatal sepsis.

Chitosan was modified through four different modification routes. First, epichlorohydrine cross-linked Chitosan was grafted with 3-Amino-1,2,4 triazole,5-thiol and melamine to produce RI and RII, respectively. Second, glutaraldehyde cross-linked chitosan was chemically modified using ammonium hydroxide then grafted with 3-Amino-1,2,4 triazole,5-thiol and melamine to produce RIII and RIV, respectively. The prepared polymers were characterized via FTIR, TGA, elemental analysis, water regain and surface area. RIII and RIV shows higher thermal stability, bigger surface area, and lower water regain, than RI and RII. Removal of Reactive Black 5 (RB5) anions from their aqueous solutions were studied using the modified chitosan adsorbents under various parameters such as pH, agitation time, and temperature. The maximum adsorption capacities are 0.492, 0.330, 0.622 and 0.698 mmol g −1 for RI, RII, RIII, and RIV, respectively, at pH 3 and 25 °C. The nature of interaction of RB5 with the adsorbents was identified. Uptake kinetics and adsorption isotherms were modeled using conventional and simple equations: best results were respectively obtained with the pseudo-second order rate equation and the Langmuir equation. The thermodynamic parameters have been calculated: the adsorption is endothermic, spontaneous and contributes to increase the entropy (randomness) of the system. RI and RII gives higher desorption yield than RIII and RIV, this probably due to the presence of the quaternary ammonium moiety in the last two sorbents.

BACKGROUND Liver fibrosis is a dynamic procedure that results from an irregularity between fibrogenesis and fibrolysis. After time this procedure can lead to cirrhosis of the liver. Liver fibrosis and cirrhosis assessment is very important for both therapeutic decisions and prognostic evaluations. In this study, we tried to use serum ferritin (SF) together with five fibrosis tests (Age-Platelet index (API), aspartate aminotransferase to alanine aminotransferase ratio (AAR), AST to platelet ratio index (APRI), Fibrosis 4 score (FIB-4), and fibro-quotient (Fibro-Q)) to assess liver fibrosis and cirrhosis and estimate possible correlation between inflammation and SF. METHODS This study was carried out on eighty-eight patients infected with HCV and twenty healthy subjects as a control. Complete blood count (CBC), aspartate aminotransferase (AST), alanine aminotransferase (ALT), antiHCV antibody, detection of HCV RNA by real-time PCR, and serum ferritin (SF) were assessed. Then API, ARR, APRI, FIB-4, and Fibro-Q were calculated. Different fibrosis stages (mild fibrosis stage (F1), moderate fibrosis stage (F2), severe fibrosis stage (F3), cirrhotic stage (F4)) were assessed using transient elastography by Fibro Scan®. RESULTS FIB-4 index was significantly elevated (p < 0.01) with the progression of liver fibrosis at F1, F2, F3, and F4 when compared to healthy control group. The APRI score elevation between F0 and F3 and between F0 and F4 was significant (p < 0.01). SF was elevated in all fibrosis stages and significantly (p < 0.01) at F3 and F4 compared to controls. CONCLUSIONS APRI coupled with SF should be the best reliable biomarkers for liver cirrhosis. Simultaneously, from our data SF involved in all stages of inflammation. Therefore, down regulation of ferritin in the early stage of fibrosis should be helpful in decreasing the inflammatory effect of ferritin.

Ficus retusa was used as reducing and stabilizing agent in the green synthesis of silver and gold nanoparticles with high dispersion stability and controllable size and shape. The controlling of reaction conditions i.e. contact time, extract quantity, metal concentration, and pH value enables the tuning of the particle size and size distribution of the metal nanoparticles. UV–visible spectroscopy was used to follow the spectral profile changes of the surface plasmon resonance of the metal nanoparticles due to different treatments. The surface plasmon resonance varies between 400 and 432 nm and between 522 and 554 nm for silver and gold nanoparticles, respectively, depending on the different reaction parameters. Atomic force and transmission electron microscopy results confirmed the success of preparation of spherical silver (15 nm) and gold (10–25 nm) nanoparticles with narrow size-distribution. Fourier transform infrared spectroscopy suggested the phenolic compounds play the key role in the reduction and stabilizing of metal ions. The colorimetric sensitivity of silver and gold nanoparticles to detect the presence of heavy metals in water was studied.

The bio-production of silver nanoparticles (Ag NPs) using Ziziphus spina-christi extract was studied as a novel, rapid, low-cost and eco-friendly route. The impact of experimental factors, such as the extract quantity, precursor concentration and pH on the size and size distribution of Ag NPs, was studied with the aid of UV–vis spectrophotometer and transmission electron microscope (TEM). The FTIR analysis was carried out to identify the functional groups in Ag NPs. The as-synthesized Ag NPs was used as a catalyst for the reduction of 4-nitrophenol (4-NP) to 4-aminophenol (4-AP) in the presence of NaBH4.

Interleukin-1β (IL-1β) assumes a centric role in the regulation of immune and inflammatory responses and thus has been recognized in immune mediated diseases like type 2 diabetes mellitus (T2DM). We aimed to investigate expressed level of IL-1β and its relation with IL-1β -511TC polymorphism in T2DM patients. This study enrolled 80 subjects (50 patients with T2DM and 30 healthy control subjects). Laboratory investigations included fasting (FBG) and 2 h postprandial blood sugar (2 h PBG), HBA1c, lipid profile, and renal function tests. Genotyping of IL-1β -511TC (rs16944) SNP assay by real-time PCR and relative quantitation of IL-1β gene expression transcript by real-time PCR.T2DM patients had significantly higher FBG and 2 h PBG, HBA1c, LDLc, TC, TG, systolic, and diastolic BP while lower HDLc compared with control group. IL 1- β -511 TC, CC genotype and C allele were significantly associated with risk of T2DM with odds ratio (OR) 4.73, 95%CI (1.21-18.39) and OR 2.27, 95%CI (1.72-4.40), respectively. Moreover, diabetic patients had significantly higher IL 1- β gene transcript compared with control group (P 0.001). CC genotype of IL 1- β -511 TC had the highest significant level of IL 1- β gene transcript demonstrated compared with C/T and T/T genotypes (P 0.001) in patients.C allele of IL-1 β -511 TC could be considered risk factor contributor to T2DM and excess level of IL-1 β transcript may disclose to some degree the inflammatory role of cytokines in T2DM.

In this study, Pimpinella anisum seeds were extracted under various conditions (solvent type, temperature, solvent/plant ratio and contact time). The potency of the resulted extracts towards biosynthesis of silver and gold nanoparticles was assessed. The most potent extract towards reduction of both Ag+ and Au3+ ions was obtained using 70% methanol at 60 °C, with a solvent/plant ratio of 10 mL/g and extraction time for 60 min. The prepared nanoparticles were structurally characterized by UV–vis, transmission electron microscope, dynamic light scattering and zeta potential analysis. Phenolics and carbohydrates present in P. anisum were characterized as the active biomolecules responsible for metal ion reduction; based on FT-IR and phytochemical analysis. Further, silver and gold nanoparticles were tested for their free radical scavenging activity against 1,1-diphenyl-2-picryl-hydrazyl (DPPH), and antimicrobial activity against Escherichia coli, Staphylococcus aureus, Aspergillus flavus and Candida albicans using disk diffusion method. Biosynthesized AgNPs showed higher antioxidant and antimicrobial activities compared to AuNPs and P. anisum extract. The foregoing results suggest that P. anisum seeds extract can be extensively used in green production of potential antioxidant and antimicrobial AgNPs for safe biomedical application.

Chitosan was cross-linked using epichlorohydrine to form chitosan gel. The resins obtained were chemically modified through the reaction with to 1,1,1,3,3,3 hexafloro,2-bis (3-amino,2-hydroxyphenyl) propane to produce resin (RI), 3-amino-1,2,4 triazole,5-thiol to produce resin (RII), and melamine to produce resin (RIII). The uptake of Reactive Black 5 (RB5) from aqueous media by the obtained resins was studied using batch method. Various parameters such as pH, agitation time, RB5 concentration and temperature were studied. The resins showed high affinity for the adsorption of RB5 where uptake values of 0.63, 0.45, and 0.33 mmol/g were reported for resins RI, RII, and RIII, respectively at 25°C. Both kinetics and thermodynamic parameters of the process were estimated. These data indicated an endothermic spontaneous adsorption process and kinetically followed the pseudo-second order model, Fickian diffusion low and Elovich equation. Desorption of RB5 from the surface of the prepared resins was efficiently d...

Chemical investigation of the chloroform extract of the Egyptian Red Sea soft coral, Heteroxenia ghardaqensis (Family Xeniidae), led to the isolation of three gorgostane derivatives, namely gorgosten-5(E)-3β-ol (1), gorgostan-3β,5α,6β, 11α-tetraol (sarcoaldosterol A) (2) and gorgostan-3β,5α,6β-triol-11α-acetate (3). To our knowledge, sterol 3 is reported in this article for the first time. The structure elucidation of these compounds was deduced by 1-D and 2-D NMR as well as ESIMS. Sterol 1 showed moderate activity as growth inhibitor of human colon tumour cell lines.

Chitosan/gluteraldehyde resin was chemically modified using ammonium hydroxide to produce (RI) resin, which was additionally semi cross-linked with epichlorohydrine through hydroxyl group of chitosan. The obtained resin was modified with 3-Amino-1,2,4 triazole,5-thiol to produce resin (RII)/or melamine to produce resin (RIII). The uptake of modified chitosan resins toward Brilliant Blue R250 (BBR250) from aqueous media was studied using batch method. Various parameters such as pH, agitation time and temperature had been studied. The resins showed high affinity for the adsorption of BBR250 from aqueous media where uptake values of 0.97, 0.79 and 2.505 mmol/g were reported for resins RI, RII and RIII at 25 °C, respectively. Both kinetics and thermodynamic parameters of the process were estimated. These data indicated an endothermic spontaneous adsorption process and kinetically followed the pseudo-second order model, Fickian diffusion low and Elovich model. Desorption of BBR250 from the prepared resins was efficiently done using sodium hydroxide.

The essential oil from aerial parts of Psoralea pubescence (Miq.) Standl (Leguminoseae) was analyzed by gas chromatography (GC) and GC/mass spectroscopy systems. The major components identified were psoralen (24.8%), bakuchiol (21.3%), β-caryophyllene (8.5%), germacrene D (6.8%), and α-humulene (4.6%). The major volatiles released by β-glucosidase treatment of the aqueous plant residue were δ-pinene (28.3%), germacrene D (13.6%), and tricyclene (10.2%). The oil showed significant antibacterial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, and Pseudomonas aeruginosa, while the β-glucosidase-liberated fraction was inactive.

Starting from (S)-aspartic, (S)-malic, (S)-citramalic and (S,R)-thiomalic acid, new types of 4,4-difluoro-substituted a-ami- no-, a-hydroxy- and a-mercaptopentanoic acids have been synthe- sized, applying hexafluoroacetone as protecting and activating reagent. The new partially fluorinated a-functionalized carboxylic acids represent interesting monomers for peptide and depsipeptide modification and for rational design and elucidation of secondary structure.

C-Sulfonyldithioformates 3 have been shown to be super-heterodienophiles in [4 + 2] cycloadditions with acyclic and cyclic dienes. Acyclic 1,3-dienes react with 3 in chloroform at room temperature to give the corresponding dihydrothiopyrans 4–6, while cyclopentadiene reacts with 3 to afford endo- and exo-2-thiabicyclo[2.2.1]heptene 7. Furthermore, the enophilic properties of 3 have been demonstrated by reacting 3 with tetramethylallene, 1-butene and trans-2-butene to afford the corresponding ene adducts 9, 10 and 11 respectively in quantitative yields.

An efficient access to L-α-methylhomoisoserine derivatives starting from L-citramalic acid is described. The new compounds are GABA derivatives and represent new, versatile building blocks for peptide and depsipeptide modification.

Efficient syntheses of l -homoisoserine and d , l -homoisocysteine derivatives starting from l -malic and d , l -thiomalic acid using hexafluoroacetone as protecting and activating agent are described. The new compounds are interesting building blocks for the preparation of non-natural peptides and depsipeptides as well as for the construction of new GABA derivatives.

3-Acetyl-4-hydroxycoumarin (2) was reacted with some aldehydes (4-chlorobenzaldehyde, 4-bromobenzaldehyde, 5-methylfurfural) to afford the chalcones (3a-c). Cyclization of these chalcones with malononitrile in the presence of ammonium acetate afforded pyridine carbonitriles (4a-c), while the cyclization reaction of chalcones (3a-c) with ethyl cyanoacetate afforded the oxopyridine carbonitriles (5a-c). On the other hand, the chalcones (3a-c) reacted with hydrazine hydrate in alcohol to yield pyrazoles (6a-c), but when the same reaction is carried out in the presence of acetic acid, the acetyl pyrazole derivatives (7a-c) were obtained. Finally, the reaction of the chalcones (3a-c) with phenylhydrazine afforded phenylpyrazole derivatives (8a-c). The structures of synthesized compounds were confirmed by their micro analysis and spectral data (IR, NMR and MS). Twelve samples were evaluated for the human breast adenocarcinoma cytotoxicity, three of them showed moderate activity, the rest of the samples showed weak cytotoxic activity (very high IC50), but for the hepatocarcinoma cell lines four samples showed weak cytotoxic effect, while the rest of the compounds showed very weak effect. For antimicrobial study, three compounds proved to be the most promising against tested bacterial organisms.

The mechanism of the formation of gem-disulfenyl dichlorides 2 from active methylene compounds 1 and sulfur dichloride (via the chlorodithio derivatives 12) has been elucidated. Reduction of 2 under a variety of conditions yields, in varying amounts, the corresponding 1,2,4,5-tetrathianes 14 with concomitant formation of the tetrasulfides 15 and/or the desulfurated disulfides 16. The pyrolysis of 2 and of the corresponding bis(disulfides) 5 leads to 14, arguably via the corresponding thiosulfines 4. When compounds 2 are treated with cyanide ions, reduction takes place rather than substitution, leading to the corresponding 1,2,4-trithiolanes 19. The halogenation of 5 leads to mixtures of hexathiocanes 17, hexathiepanes 18, and tetrathiolanes 7 which, however, could not be obtained in pure form. The single-crystal structures of the key compounds 2a, 5ad, 5bd, and 16b have been determined by X-ray diffraction.

This review covers the preparation and reactions of carbon chloride sulfides, based on online CAS and Beilstein searches. One hundred and thirty-five compounds are listed together with 238 literature references. A section on unreported compounds with the composition CxClySz is also included.

A novel series of pyrrolothiazines 2 – 4 and pyrrolopyrimidines 5 – 7 have been synthesized. The structures of these compounds were established by spectroscopic and element microanalytical data. The newly synthesized compounds were evaluated as inhibitors of TSG-14. The most effective results were obtained by the S -sec-butyl derivatives 6e (80%) and the N -ethyl derivatives 4e (70%).

2-Phenyl-4-p-tolylhydrazono-2-oxazoline-5-one (3) was rearranged by the action of phenols and naphthols into 1,2,4-triazole-5-carboxylic esters (5) that were rearranged further on reflux in AcOH-ZnCl2 into triazolyl ketones (7). Rearrangement of 3 into 1,2,4-triazole derivatives could also be effected by the action of heterocyclic amines and 1-naphthylamine. © John Wiley & Sons, Inc.

Investigation of the aqueous alcoholic extract of Pyrus calleryana Decne. leaves led to the isolation of two new phenolic acids glycosides, namely protocatechuoylcalleryanin-3- O -β-glucopyranoside ( 1 ) and 3′-hydroxybenzyl-4-hydroxybenzoate-4′- O -β-glucopyranoside ( 2 ), together with nine known compounds among them lanceoloside A and methylgallate, which have been isolated for the first time from the genus Pyrus . Structures of the isolated compounds were established by spectroscopic analysis, including UV, IR, HRESI-MS, and 1D/2D NMR. The total extract and some isolated compounds were determined against DPPH (2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydrazinyl radical, for their free radical scavenging activity, the total alcoholic extract showed strong antioxidant activity while the two new compounds showed weak antioxidant activity.

The present study aimed to investigate the chemical composition, and the antioxidant and antiproliferative activities of Ailanthus excelsa, a plant used in Egyptian traditional medicine. Chromatographic separation of a methanol extract of A. excelsa leaves yielded four fl avones, namely apigenin (1), apigenin 7-O-β-glucoside (2), luteolin (3), and luteolin 7-O-β-glucoside (4), and seven fl avonols, namely kaempferol (5), kaempferol 3-O-α-arabinoside (6), kaempferol 3-O-β-galactoside (7), quercetin (8), quercetin 3-O-α-arabinoside (9), quercetin 3-O-β- galactoside (10), and quercetin 3-O-rutinoside (11). The A. excelsa extract tested in different in vitro systems (DPPH and FRAP assays) showed significant antioxidant activity. The potential antiproliferative activity of the A. excelsa extract and isolated flavonoids against five human cancer cell lines such as ACHN, COR-L23, A375, C32, and A549 was investigated in vitro by the SRB assay in comparison with one normal cell line, 142BR. The extract exhibited the highest inhibitory activity against C32 cells with an IC50 value of 36.5 μg ml-1. Interesting activity against COR-L23 was found with 10 (IC50 value of 3.2 μg ml-1). Compounds 1 and 3 inhibited cell growth in both amelanotic melanoma and malignant melanoma cells.

The reaction of active methylene reagents Ia-Ie with phenyl isothiocyanate in basic N,N-dimethylformamide solution followed by cyclization with ethyl cyanobromoacetate II affords the acyclic thioether derivatives IVa-IVe. The use of IVa-IVe in heterocyclic synthesis was described.

The reaction of ethyl 2-arylhydrazono-3-oxobutyrates (Ia, Ib) with active methylene ketones afforded pyridazin-5-carbonitrile derivatives. The methyl function in the ethyl pyridazin-3-carboxylate derivatives IIa, IIb reacted with arylidenemalononitrile to yield the phthalazine derivatives Va-Vf and with elemental sulfur to yield the thienopyridazines XIXa, XIXb. The cinnolines are producted from reaction of IIa, IIb with diethyl acetonedicarboxylate.

Substituted pyridin-2-thiones, 2-pyridones, thiopyrans and pyranoazoles could be synthesized via the reaction of 2-thiocarbamoyl cinnamonitriles with some active methylene reagents.

Synthese de [thenylidene-2]-3 aryl-5 3H-furannones-2 (A) a partir de thiophenecarbaldehyde-2 et d'acides aroyl-3 propioniques; reactions de A avec l'ammoniac (obtention de pyrroline-2ones-5), avec l'hydrazine (obtention d'hydrazides d'acides α-aroyl thiopheneacryliques-2 qui se cyclisent en 2H-pyridazones-3. Etude biologique

N-(9H-Xanthen-9-yl)succinimide (1) is prepared by the reaction of xanthene with N-bromosuccinimide. Hydrolysis of 1 with 5% NaOH yields 3-[(9H-xanthen-9-yl)aminocarbonyl]propionic acid (3a). The corresponding methyl ester 3c is obtained from 3a by the action of diazomethane. The butanol derivative 4a can be obtained by reduction of 3a or 3c with LiAlH4. Treatment of 1 with LiAlH4 yields the pyrrolidine derivative 5. N-(9H-Xanthen-9-yl)phthalimide (2) undergoes similar reactions like its analogue 1.

N-(9H-Xanthen-9-yl)succinimide (1) is prepared by the reaction of xanthene with N-bromosuccinimide. Hydrolysis of 1 with 5% NaOH yields 3-[(9H-xanthen-9-yl)aminocarbonyl]propionic acid (3a). The corresponding methyl ester 3c is obtained from 3a by the action of diazomethane. The butanol derivative 4a can be obtained by reduction of 3a or 3c with LiAlH4. Treatment of 1 with LiAlH4 yields the pyrrolidine derivative 5. N-(9H-Xanthen-9-yl)phthalimide (2) undergoes similar reactions like its analogue 1.