Synthesis and In Vitro Cytotoxic Activity of Novel Triazole‐Isoxazole Derivatives

New derivatives of triazole‐isoxazole were synthesized through a four‐step reaction starting from various ethyl 4‐aryl‐2,4‐dioxobutanoate derivatives. Finally, all compounds were examined by MTT assays for cytotoxic activity in two human breast cancer cell lines (MCF‐7 and T‐47D).     

Synthesis and evaluation of antiproliferative activity of substituted N-(9-oxo-9H-xanthen-4-yl)benzenesulfonamides

Several novel N-(9-oxo-9H-xanthen-4-yl)benzenesulfonamide derivatives were prepared as potential antiproliferative agents. The in vitro antiproliferative activity of the synthesized compounds was investigated against a panel of tumor cell lines including breast cancer cell lines (MDA-MB-231, T-47D) and neuroblastoma cell line (SK-N-MC) using MTT colorimetric assay. Etoposide, a well-known anticancer drug, was used as a positive standard drug. Among synthesized compounds, 4-methoxy-N-(9-oxo-9H-xanthen-4-yl)benzenesulfonamide (5i) showed the highest antiproliferative activity against MDA-MB-231, T-47D, and SK-N-MC cells. Furthermore, pentafluoro derivatives 5a and 6a exhibited higher antiproliferative activity than doxorubicin against human leukemia cell line (CCRF-CEM) and breast adenocarcinoma (MDA-MB-468) cells. Structure–activity relationship studies revealed that xanthone benzenesulfonamide hybrid compounds can be used for the development of new lead anticancer agents.     

Synthesis and labeling of p-NH2-Bn-DTPA-(Dabcyl-Lys6,Phe7)-pHBSP with 99mTc as a radiopeptide scintigraphic agent to detect cardiac ischemia

Journal of Radioanalytical and Nuclear Chemistry - Myocardial ischemia and infarction represent a major health burden worldwide, but their immediate diagnosis can reduce mortality and healthcare...     

Single Cell Protein Production by <Emphasis Type="Italic">Saccharomyces cerevisiae</Emphasis> Using an Optimized Culture Medium Composition in a Batch Submerged Bioprocess

Saccharomyces cerevisiae PTCC5269 growth was evaluated to specify an optimum culture medium to reach the highest protein production. Experiment design was conducted using a fraction of the full factorial methodology, and signal to noise ratio was used for results analysis. Maximum cell of 8.84 log (CFU/mL) was resulted using optimized culture composed of 0.3, 0.15, 1, and 50 g L^?1 of ammonium sulfate, iron sulfate, glycine, and glucose, respectively at 300 rpm and 35 °C. Glycine concentration (39.32 % contribution) and glucose concentration (36.15 % contribution) were determined as the most effective factors on the biomass production, while Saccharomyces cerevisiae growth had showed the least dependence on ammonium sulfate (5.2 % contribution) and iron sulfate (19.28 % contribution). The most interaction was diagnosed between ammonium sulfate and iron sulfate concentrations with interaction severity index of 50.71 %, while the less one recorded for glycine and glucose concentration was equal to 8.12 %. An acceptable consistency of 84.26 % was obtained between optimum theoretical cell numbers determined by software of 8.91 log (CFU/mL), and experimentally measured one at optimal condition confirms the suitability of the applied method. High protein content of 44.6 % using optimum culture suggests that Saccharomyces cerevisiae is a good commercial case for single cell protein production.     

Novel (thio)barbituric-phenoxy-N-phenylacetamide derivatives as potent urease inhibitors: synthesis,in vitro urease inhibition,and in silico evaluations

Structural Chemistry - A novel series of (thio)barbituric-phenoxy-N-phenylacetamide derivatives 7a-l was synthesized and evaluated against Helicobacter pylori urease. The latter assay revealed that...     

Novel and facile methods for the synthesis of DTPA-mono-amide: a new completely revised strategy in radiopharmaceutical chemistry

DTPA is a very strong metal chelator widely utilized in radiopharmaceutical chemistry for conjugation of chemicals which do not have enough potency for direct metalo-labeling and also to manage toxic radioactive materials such as plutonium, americium, and curium. It is difficult to conjugate DTPA to an amine group in a singular direction and such reactions usually also coincidently produce a mixture of DTPA-bis-amides and DTPA-mono-amide resulting in considerable insufficiencies/difficulties in synthesis and especially yield/separation procedures. In this paper, novel methods for the exclusive synthesis of DTPA-mono-amide have been established which extensively reduce the difficulties otherwise encountered and increase the reaction’s yield considering the green chemistry approaches. This is expected to be of interest to radiopharmaceutical researchers interested in the DTPA (Radio)-metallic-conjugate. Overall, this paper provides a framework to achieve a higher degree of propriety from DTPA as a chelator to conjugate to the chemical compounds.     

Synthesis and characterization of nanostructured-segmented block copolyetheramide based on nylon6 and poly(ethylene oxide)

<正>Segmented block copolymer based on nylon6(N6) and polyethylene oxide(PEO) with stochiometric ratio was synthesized via a two-step process.The first step represents end capping of N6 in the presence of adipic acid leading to carboxy terminated N6,and the second one is polycondensation of the latter product with PEO in the presence of catalyst and thermostabilizer to form a high molecular weight multi-block copolymer.Several methods were applied to characterize the synthesized copolymer such as Fourier transform infrared spectroscopy,proton nuclear magnetic resonance spectroscopy,differential thermal analysis,differential scanning calorimetry,X-ray diffraction and atomic force microscopy. The obtained results confirmed the multi-block structure for copolymer with a very high degree of micro-phase separation. Atomic force microscopy micrographs indicated that the morphology was the dispersion of high stiffness nanostructured polyamide(PA) domains in the amorphous region of PEO matrix,which can be very important in their performance for membrane processes.     

Synthesis of 4,4′-diaminotriphenylmethane derivatives using H3PW12O40 and HZSM5 zeolite under solvent-free conditions

An efficient and very simple method for synthesis of 4,4′-diaminotriphenylmethane and its derivatives has been achieved via reaction of various substituted aromatic aldehydes containing both electron-donating and electron-withdrawing groups with various anilines having electron-withdrawing and electron-donating groups in the presence of catalytic amounts of HZSM5 zeolite and H₃PW₁₂O₄₀ under solvent-free conditions. The reaction proceed with shorter reaction time and higher yield compared to the results obtained in different solvents. Anilines having electron-donating groups in comparison with those having electrondonating group performed this transformation in better yields. Also the results show that the steric hindrance plays an important role in this transformation. Reusability is an advantage of the HZSM5 zeolite, while it showed lesser activity than H₃PW₁₂O₄₀. The one-pot reaction, simple work up, high yields, use of efficient catalytic amount and eco-friendly reagents are the advantages of the proposed method. All products were characterized using ¹H NMR, ¹³C NMR and IR.