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Novel pyrazolyl 2-hydroxychalcone derivatives 3a–e and pyrazolylpyrazoline derivatives 4a–e and 5a–j derived from the naturally existing furochromone (Khellin) were synthesized and evaluated for th...

Pure Fe3O4 and NiFe2O4 nanoparticles were synthesized and successfully coated with chitosan (CS). XRD patterns confirmed the formation of a pure spinel Fe3O4 and NiFe2O4 structure without presence of any other phases. TEM results revealed that the Fe3O4 and NiFe2O4 nanoparticles were 19.5 and 7.3 nm in size, respectively, with a good homogenous dispersion. The modification using chitosan did not result in a phase change. The binding of chitosan to the Fe3O4/ NiFe2O4 nanoparticles was also demonstrated by the measurement of Fourier transform infrared spectra and thermogravimetric analysis. Magnetic measurements revealed that the saturated magnetization (Ms) was 77.6, 46.2, 8.42, and 49.8 emu/g for Fe3O4, NiFe2O4, Fe3O4/CS, and NiFe2O4/CS, respectively, which are also characteristics of superparamagnetic behavior. Exposure of breast MCF-7, liver HepG2, lung A549, and colon HCT116 human cancer cell lines to the prepared compounds (0–500 μg/mL; 48 h) has resulted in a dose-dependent inhibition of cell...

3-(2-(4-methoxyphenylcarbamothioyl)hydrazinyl)-3-oxo-N-(thiazol-2-yl)propan-amide (H4L) has been synthesized and its structure has been confirmed by elemental analysis, IR, mass, and 1H and 13C NMR spectroscopy. This ligand has been used to synthesize complexes with Cu2+, V(IV)O2+, Co2+, Mn2+, and Ni2+. The structures of these complexes have been verified by elemental analyses, molar conductivities, magnetic measurements as well as UV–VIS, IR, 1H-NMR spectroscopy. The IR spectra showed that H4L acts as a uni-negative tetradentate or bidentate ligand. The molar conductance measurements proved that all complexes are nonelectrolytes except complexes 2 and 3. Moreover, the metal complexes geometrical arrangements were square planar, tetrahedral, square-pyramidal, or octahedral. The structures are consistent with the IR, UV–VIS, ESR, as well as conductivity measurements. The antiproliferative activity of the synthesized complexes against human breast adenocarcinoma MCF-7 cell line showed exploited pote...

The optimal conditions for the production of l -methionine γ-lyase (MGL) by a soil bacterium, Streptomyces DMMMH60, were established and their effects were compared using Plackett–Burman design (PBD). Accordingly, the optimal conditions of beet molasses, yeast extract, l -methionine, MgCl2, Tween 80, initial pH, aeration, temperature, inoculum size and incubation period for the maximum MGL production (60.7 U/mg) were 23.5 g/L, 0.79 g/L, 0.87 g/L, 0.85 g/L, 0.41%, 8.3, 50 ml, 33 °C, 5.2 ml, and 4 day, respectively. Initial pH was found to be the most significant factor for the production of MGL based on the calculated percentage of participation P (%) from an analysis of the variance (ANOVA). Additionally, MGL was purified from the supernatant of S. DMMMH60 using heat treatment, DEAE-cellulose and Sephadex G100, and the purified enzyme displaying 3.15-fold in comparison with the crude enzyme. Purified enzyme exhibiting a single band of 55 kDa subunits on the SDS-PAGE and the enzyme had maximum activity in pH 8 at 45 °C with ionic stability within pH range 6.5–8.5 and thermal stability below 60 °C. In-vitro, MGL showed a significant cytotoxic effect against cancer cell lines whereas those for normal cells was demonstrated a negligible toxicity.

A one-pot reaction of 6-methyl-3-thioxo-3,4-dihydro-[1,2,4]triazin-5-one 1 with selected aldehydes 2a-d and chloroacetic acid afforded the respective 2-arylidene-6-methyl-thiazolo[3,2-b][1,2,4]triazine-3,7-diones 4a-d. Compunds 4a-d could be also obtained via the reaction of 1 with chloroacetic acid in refluxing acetic acid to give 6-methyl-thiazolo[3,2-b][1,2,4]triazine-3,7-dione 3 then, Knoevenagel condensation of 3 with aldehydes 2a-d gave compounds 4a-d. Heterocyclization of 4a-c with hydrazine hydrate and phenylhy- drazine gave the corresponding pyrazolines 5a-c and 6a-c, respectively. Moreover, 7-amino-9-(aryl)-3-methyl-2-oxo-2H-pyrido[2',3':4,5][1,3]thiazolo[3,2-b][1,2,4]triazine-8-carbonitrles 7a-c were synthesized by the reaction of 4a-c with malononitrile in the presence of ammonium acetate. The structures of newly synthesized compounds were confirmed by analytical and spectroscopic measurements. Some selected new compounds were screened for their cytotoxic activities against three human cancer cell lines (HepG2, MCF-7 and A549) using SRB assay and the structure-activity relationship (SAR) was discussed. The biochemical assays including antioxidant enzyme, oxidative stress and estimation of nucleic acids and proteins have been discussed for some selected compounds. The molecular docking of 4c and 7b has been also studied.

Some cyclic and acyclic nucleosides of thieno[2,3-d]-pyrimidine derivatives were synthesized via the reaction of compounds 1 and 2 or 3 and 4 with 2-chloroethyl methyl ether or 2,3,4, 6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide. Nucleosides 9, 10, 15, and 16 were tested as antiviral agents against herpes simplex virus type-1 (HSV-1) and hepatitis-A virus (HAV). Compound 15 showed the highest effect on HSV-1 than the other three compounds, while the four tested compounds did not show any activity against HAV.

Thiosemicarbazone ligand, 2-((4,9-dimethoxy-5-oxo-5H-furo[3,2-g]chromen-6-yl)methylene) hydrazinecarbothioamide and its Cd(II), Cu(II), Zn(II), Ni(II), Co(II), VO(II), and Mn(II) complexes have been prepared and characterized by various spectroscopic and analytical techniques. Complexes molar conductance measurements displayed that all complexes (2–8) are non-electrolyte. With general composition [M(H3L)(CH3COO)2H2O].nH2O, where M = Cd(II), Cu(II), Zn(II), Ni(II), Co(II) and Mn(II) while complex (8) has [VO(H3L)(SO4)H2O].2H2O formula. Based on analytical and spectral measurements, the octahedral or distorted octahedral geometries suggested for complexes. Ligand and complexes anti-proliferative activities were assessed against three various human tumor cell lines including breast cancer (MCF-7), liver cancer (HepG2) and lung cancer (A549) using SRB fluorometric assay and cis-platin as positive control. The anti-proliferative activity result indicated that the ligand and its complexes have considerable anti-proliferative activity analogous to that of ordinarily utilized anti-cancer drug (cis-platin). They do their anti-cancer activities by modifying free radical's generation via raising the superoxide dismutase activity and depletion of intracellular reduced glutathione level, catalase, glutathione peroxidase activities, escorted by highly generation of hydrogen peroxide, nitric oxide and other free radicals leading to tumor cells death, as monitoring by decreasing the protein and nucleic acids synthesis.

Background: This study was aimed to evaluate protective and therapeutic effects of a specific mixture, containing vitamin C, lysine, proline, epigallocatechin gallate and zinc, as well as alpha-1-antitrypsin protein on lung tumorigenesis induced by benzo(a) pyrene [B(a)P] in mice. Materials and Methods: Swiss albino mice were divided into two main experiments, experiment (1) the mice were injected with 100 mg/kg B(a)P and lasted for 28 weeks, while experiment (2) the mice were injected with 8 doses each of 50 mg/kg B(a)P and lasted for 16 weeks. Each experiment (1 and 2) divided into five groups, group (I) received vehicle, group (II) received the protector mixture, group (III) received the carcinogen B(a)P, group (IV) received the protector together with the carcinogen (simultaneously) and group (V) received the carcinogen then the protector (consecutively). Results: Total sialic acid, thiobarbituric acid reactive substances, vascular epithelial growth factor, hydroxyproline levels, as well as elastase and gelatinase activities showed significant elevation in group (III) in the two experiments comparing to control group (P < 0.001). These biochemical alterations were associated with histopathological changes. Administration of the protector in group IV and group V causes significant decrease in such parameters with improvement in histopathological alterations with improvement in histopathological alterations when compared with group III in the two experiments (P < 0.001). Conclusion: The present protector mixture has the ability to suppress neoplastic alteration and restore the biochemical and histopathological parameters towards normal on lung carcinogenesis induced by benzo(a) pyrene in mice. Furthermore, the present mixture have more protective rather than therapeutic action.

In this study, extracts of the flowers of the folk medicinal plant Bombax malabaricum DC were biologically and chemically screened. Chemical constituents in the n-hexane fraction from the flowers of B. malabaricum DC were investigated using gas-liquid chromatography (GLC) analysis, affording 14 compounds, including cholesterol, stigmasterol, campesterol and α-amyrin, while the residual 10 compounds are hydrocarbons. GLC analysis of the fatty acid (FA) esters established the majority abundance of the saturated FA over their unsaturated analogues. The polar methanol fraction afforded seven flavones: vicenin 2 (1), linarin (2), saponarin (3), cosmetin (4), isovitexin (5), xanthomicrol (6) and apigenin (7). Structures 1-7 were established by intensive studies of various spectral data (H-NMR, mass spectroscopy and UV) and comparison with authentic samples. Compounds 1-7 are described here for the first time from this plant. Extracts of n-hexane and methanol exhibited significant antioxidant and antimicrobial activities.