The preparation of a magnetically recoverable and reusable Fe3O4@benzothiazole-Cu(II) nanoparticles with their catalytic and electrochemical sensing properties are reported in this manuscript. The prepared Fe3O4@benzothiazole-Cu(II) nanoparticles are characterized using various analytical techniques, including XRD, FTIR, SEM, TEM, XPS, TGA and VSM analysis. The prepared system has shown good catalytic activity in the reduction of 2-NBA, achieving a reaction rate constant of 0.093 min−¹ in 2 min with a low catalyst loading. The synthesized catalyst also showed very high efficiency in the reduction of 4-nitro-phenol and methylene blue within 13 min and 4 min, respectively. The prepared material demonstrated good recovery yield and could be reused as a catalyst for multiple cycles without a significant loss in catalytic activity. It also exhibited a remarkable electrochemical sensing capability for the detection of ascorbic acid, H2O2, and paracetamol at various concentrations, as determined through cyclic voltammetry and impedance measurements. They exhibited clear redox transformations, indicating the electrochemical sensing ability of the prepared materials.

In the present study, the aqueous seed extract of an Origanum marjorana plant and the fruit rind extract of a Garcinia indica plant were used to prepare ZnO nanoparticles. The antimicrobial effects of the prepared nanoparticles on bacterial pathogens and their antiproliferative effects on the HCT 116 cancer cell line were evaluated, with a specific focus on colon cancer. The prepared ZnO nanoparticles were characterized via XRD, SEM, FTIR, and UV‒Vis spectroscopy. The antibacterial activities of the synthesized nanoparticles were studied against both the gram-positive and gram-negative microorganisms B. cereus and S. typhi. These compounds presented moderate activity compared with the standard ciprofloxacin. The MICs for OM-ZnO were 2 µg/mL for S. typhi and 2 µg/mL for B. cereus. For GI-ZnO, 4 µg/mL for S. typhi and 4 µg/mL for B. cereus were observed. These results confirmed that the antibacterial efficacy of the nanoparticles depends on their concentration. The antiproliferative effects of the ZnO nanoparticles were evaluated using the MTT assay and cell cycle analysis. ZnO nanoparticles showed good antiproliferative effects on the tested cell lines. Studies on the cell cycle have suggested that ZnO nanoparticles effectively induce cell cycle arrest at the G2/M phase and trigger apoptosis. Compared with untreated HCT 116 cells (9.31

In the present work, copper (II) immobilized on guanidine functionalized Fe3O4 nanoparticles (Fe3O4@Guanidine–CuII) are developed as a heterogeneous catalyst. Fe3O4@Guanidine–CuII is well-characterized by adopting FT-IR, XRD, SEM, TEM, EDX, SEM-elemental mapping, TG–DTA, XPS, ICP-OES, and VSM analysis. Fe3O4@Guanidine–CuII is employed for the selective reduction of nitro group on electronically diversified nitroarenes involving NaBH4 to serve as a hydrogen source in ethanol medium. Anilines resulted from the reduction of nitroarenes are of excellent yields with high TON and TOF numbers, indicating the efficiency of the prepared catalyst. Also, the catalyst has been recovered with effective yield over the time of the reaction, and the recovered catalyst was used up to eight cycles for the reaction without any significant change in the catalytic activity. This notable feature of the prepared catalytic system makes it highly promising, not only for an industrial but also from an environmental point of view.

In the present study, we are reporting a simple and efficient method for the one‐pot synthesis of the biologically important heterocyclic molecules 5‐unsubstituted 3,4‐dihydropyrimidin‐2‐ones and thiones using gem‐dibromomethylarenes, oxalacetic acid, and urea or thiourea. Gem‐dibromomethylarenes are used as aldehyde equivalent for the efficient synthesis of 3,4‐dihydropyrimidin‐2‐ones/thiones. This reaction offers advantages for the synthesis of these compounds, including ready availability of the starting materials, experimental simplicity and in good yields. Besides, the synthesized molecules are interesting for their biological and pharmacological actions.

1,2,4-Oxadiazole is one of the most promising heterocyclic ring systems in medicinal chemistry. In the present paper, we report the method for an efficient one-pot synthesis of 3,5-diaryl substituted 1,2,4-oxadiazoles using a two-component reaction of gem-dibromomethylarenes with amidoximes in good yields. In this method, gem-dibromomethylarenes are used as benzoic acid equivalents for the efficient synthesis of aryl-substituted 1,2,4-oxadiazoles. It is anticipated that this methodology will have versatile applications in the practical syntheses of various molecules of both medicinal and material chemistry importance.

Background: Biginelli reaction is one of the most important multiple-component chemical reactions which creates 3,4-dihydropyrimidin-2(1H)-ones. Even though Biginelli reaction was reported over a century using different substrates, literature lacks the example of the use of alcohols as a substrate. The substitution of aldehyde component with another functional group has not been explored so far. Method: In the present study, we have used Propylphosphonic anhydride (T3P (R))-DMSO as an efficient and mild reagent for the one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones/thiones from aromatic alcohols. Results: Alcohols are oxidized in situ to aldehydes under mild conditions, which in turn undergo a three-component reaction with beta-ketoester and urea/thiourea to afford 3,4-dihydropyrimidin-2(1H)ones/thiones. Conclusion: The synthesis of 3,4-dihydropyrimidin-2(1H)-ones/thiones directly from alcohols has been reported for the first time under mild reaction conditions in good yield. Easy work up procedure, low cost and less toxicity of the reagent are the main advantages of this protocol.

A series of novel N -(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)piperidine-4-carboxamide derivatives 10 ( a – f ), 12 ( a – c ) and 14 ( a – c ) were synthesized and characterized by FTIR, 1 H-NMR, mass spectral and elemental analysis. The efficacy of these derivatives to inhibit in vivo angiogenesis was evaluated using chick chorioallantoic membrane (CAM) model and their DNA cleavage abilities were evaluated after incubating with calf thymus DNA followed by gel electrophoresis. These novel piperidine analogues efficiently blocked the formation of blood vessels in vivo in CAM model and exhibited differential migration and band intensities in DNA binding/cleavage assays. Among the tested compounds 10a , 10b , 10c , 12b , 14b and 14c showed significant anti-angiogenic and DNA cleavage activities compared to their respective controls and the other derivatives used in this study. These observations suggest that the presence of electron donating and withdrawing groups at positions 2, 3 and 4 of the phenyl ring of the side chain may determine their potency and as anticancer agents by exerting both anti-angiogenic and cytotoxic effects .

The normal female reproductive hormone estrogen has been linked with increased risk of breast and many other forms of cancer. This is largely due to metabolic conversion of estrogens into highly reactive catechol estrogen quinones which can interact with DNA and cause a variety of DNA adducts and lesions. Detection and analysis of these adducts and their associated cellular responses involve complex chemical, enzymatic, and LC-MS based methods, which are both laborious and require specialized expertise and instrumentation. Herein, we show that using a biotin-labeled estradiol allows immunodetection of estrogen-induced DNA adducts by slot blot and single-cell molecular combing and proximity ligation assays. The biotinylated and unlabeled estradiols induced similar levels of DNA single and double strand breaks as measured by comet assays. Using biotinylated estrogen, we further show that estrogens are able to activate the Fanconi anemia-BRCA tumor suppressor pathway and cause DNA strand breaks and oxidatively modified DNA bases as well as gross chromosomal aberrations. Utilization of biotin-labeled estrogens could be a powerful tool to detect estrogen adducts and associated DNA damage, and to track estrogen adduct-induced cellular responses and carcinogenic mechanisms in cultured cells. The techniques presented here allow simple and rapid detection and quantitation of estrogen adducts by slot blot as well as direct visualization on the DNA strand and could pave the way for developing new treatments to protect the genome from the effects of reactive estrogen metabolites. © 2016 Wiley Periodicals, Inc.

A novel series of building blocks consisting of 6-methyl-N 1 (4-(pyridin-3-yl)pyrimidin-2-yl)benzene-1,3-diamine have been synthesized as potential antiproliferative agents. Compounds 10c, 12d and 14a with an electron releasing substituent at the ortho and para position on the phenyl ring showed excellent in vitro potency against tested human leukemia cells (K562 and Reh) with IC50 values range from 2.3 to 5.3 μM.

A series of novel 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one aliphatic/ aromatic/ heterocyclic amine derivatives were synthesized in good yield. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesized compounds were screened for their in vitro antibacterial activity by agar well diffusion and micro dilution method against standard strains of Gram-Positive (Bacillus Subtilis MTCC 121 and Staphylococcus epidermidis 435), and Gram-negative (Xanthomonas Campestris 7903 and Pseudomonas aeruginosa MTCC 7908) bacteria. Compounds with substituted heterocyclic piperazine moiety showed good activity. In particular, compound 6i showed two fold better activity compared to the standard drug Strepyomycin sulphate.

A simple and convenient procedure for the synthesis of nitriles by dehydration of aldoximes using a PCC (pyridiniumchlorochromate) has been developed. A variety of aromatic, heteroaromatic, and aliphatic aldoximes are converted. Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications (R) for the full spectral details.

A series of novel 2‐(4‐(2,4‐dimethoxybenzoyl)phenoxy)‐1‐(4‐(3‐(piperidin‐4‐yl)propyl) piperidin‐1‐yl)ethanone derivatives 9(a–e) and 10(a–g) were synthesized and characterized by 1H NMR, IR, mass spectral, and elemental analysis. These novel compounds were evaluated for their antileukemic activity against two human leukemic cell lines (K562 and CEM) by using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazoliumbromide assay. Some of the tested compounds showed good antiproliferative activity with IC50 values ranging from 1.6 to 8.0 μm. Compound 9c, 9e, and 10f with an electron‐withdrawing halogen substituent at the para position on the phenyl ring showed excellent in vitro potency against tested human leukemia cells (K562 and CEM).

The one-pot synthesis of aryl oximes is reported by the reaction of methyl arenes with NBS using hydroxyl amine hydrochloride. The direct conversion of methyl group into oxime group has been achieved under mild reaction conditions in the presence of sensitive functional groups including chloro, bromo, cyano, hydroxy, fluoro, dioxaborolane, esters, and trifluoro methyl substituents with excellent yields. The simple experimental procedure and easy purification make this protocol advantageous.

A series of novel homopiperazine derivatives were synthesized and characterized using 1H NMR, LC MS, IR and elemental analysis data. These novel molecules were evaluated for their antiproliferative activity against Reh, leukemia cells using trypan blue and MTT assays. All the molecules showed cytotoxicity with IC50 values between 50-100 μM as calculated by trypan blue assay and greater than 100 μM as calculated by MTT assay. Compound 6b with 3,5-dinitro substituents on phenyl ring of the aryl carboxamide moiety attached to homopiperazine ring showed good activity with IC50 value of 41 μM.

One-pot synthesis of 2-aryl benzothiazoles from gem-dibromomethylarenes using 2-aminoarylthiols is described. Benzothiazoles were obtained in high chemical yields under mild conditions. This transformation would facilitate synthesis by short reaction times, large-scale synthesis, easy and quick isolation of the products, which are the main advantages of this procedure.

A series of novel 2-methyl-3-(2-(piperazin-1-yl)ethyl)-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one sulfonamide and carboxamide derivatives were synthesized in good yield. The synthesized compounds were characterized by H-1-NMR, FTIR and elemental analysis. All the synthesised compounds were screened for their in vitro antimicrobial activity by agar well diffusion and micro dilution method against standard strains of Gram-positive (Bacillus subtilis MTCC 121, Staphylococcus epidermidis 435), and Gram-negative (Xanthomonas campestris 7903 and Pseudomonas aeruginosa MTCC 7908) bacteria. Compound 7a and compound 8d with dichloro substitution among sulphonamide and carboxamide series respectively showed potent inhibitory activity.

A series of novel 2-amino-6-ethoxybenzothiazole thiourea derivs. were synthesized by nucleophilic substitution reaction of 2-amino-6-ethoxybenzothiazole with different arom. isothiocyanates with good yield. The synthesized compds. were characterized by 1H-NMR, FTIR and elemental anal. In the present study, the compds. exhibited in vivo inhibition of Ehrlich Ascites Tumor (EAT) cell growth and increased the Median Survival Time (MST) and % ILS of EAT bearing mice. Further treatment of derivs. in vivo resulted in redn. of EAT cell no. and ascites formation. The efficacy of the derivs. to inhibit the angiogenesis in vivo was evaluated in tumor bearing mice peritoneum and changes in morphol. assay. The compds. suppressed the blood vessel formation in vivo in mice peritoneum and changes in morphol. Among the compds. studied, o-FC6H4- and o-MeOC6H4-substituted thiourea derivs. demonstrated highest tumor inhibitory and antiangiogenic effects against mouse tumor. [on SciFinder(R)]

In search of new anticancer agents, a series of novel 1-benzhydryl-4-(substituted phenylcarboxamide / carbothioamide)-1,4-diazepane derivatives were designed, synthesized and characterized using 1H NMR, LCMS and elemental analysis. These molecules were evaluated for their anti-cancer activity by trypan blue exclusion and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on B-cell leukemic cell line, Reh. Carboxamide moiety containing derivatives showed good activity compared to the corresponding carbothioamide derivatives. In particular, 4-benzhydryl-N-(3-chlorophenyl)-1,4-diazepane-1-carboxamide showed good activity with IC50 value of 18 µM.