An Efficient Four‐component Synthesis of Spiro[indoline‐pyrazolo[4′,3′:5,6]pyrido[2,3‐d]pyrimidine]triones

A four‐component reaction in the presence of Alum [KAl(SO₄)₂·12H₂O] as an inexpensive and reusable catalyst using the ionic liquid as an effective green reaction media is reported.     

A Novel Method for the Synthesis of Spiro[indoline‐Pyrazolo[4′,3′:5,6]pyrido[2,3‐d]pyrimidine]triones by Alum as a Reusable Catalyst

Synthesis of spiro[indoline‐pyrazolo[4′,3′:5,6]pyrido[2,3‐d]pyrimidine]trione derivatives by a cyclo‐condensation reaction of indolin‐2‐ones, barbituric acids, and 1,3‐diphenyl‐1H‐pyrazol‐5‐amines with the ionic liquid as an effective green reaction media and in the presence of Alum as a reusable catalyst was reported. Excellent yields of products, green media, use of a reusable catalyst, and short reaction time are the main advantages of this new method.     

Anticancer and DNA Binding Activities of Platinum (IV) Complexes; Importance of Leaving Group Departure Rate

The two six-coordinate Pt(IV) complexes, containing bidentate nitrogen donor/methyl ligands with general formula [Pt(X)₂Me₂(^tbu₂bpy)], where ^tbu₂bpy = 4,4′-ditert-butyl-2,2′-bipyridine and X = Cl (C₁) or Br (C₂), serving as the leaving groups were synthesized for evaluation of their anticancer activities and DNA binding properties. To examine anticancer activities of the synthetic complexes, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and ethidium bromide/acridine orange (EB/AO) staining method were performed. The binding properties of these complexes to DNA and purine nucleotides were examined, using different spectroscopic techniques. These complexes demonstrated significant anticancer activities against three cancer cell lines Jurkat, K562, and MCF-7. On the basis of the results of EB/AO staining, C₁ and C₂ were also capable to induce apoptosis in cancer cells. These complexes comprise halide leaving groups, displaying different departure rates; accordingly, they demonstrated slightly dissimilar anticancer activity and significantly different DNA/purine nucleotide binding properties. The results of DNA interaction studies of these complexes suggest a mixed-binding mode, comprising partial intercalation and groove binding. Overall, the results presented herein indicate that the newly synthesized Pt(IV) complexes are promising class of the potential anticancer agents which can be considered as molecular templates in designing novel platinum anticancer drugs. This study also highlights the importance of leaving group in anticancer activity and DNA binding properties of Pt(IV) complexes.     

Accurate Sensitivity of Quantum Dots for Detection of HER2 Expression in Breast Cancer Cells and Tissues

Here we introduce novel optical properties and accurate sensitivity of Quantum dot (QD)-based detection system for tracking the breast cancer marker, HER2. QD525 was used to detect HER2 using home-made HER2-specific monoclonal antibodies in fixed and living HER2⁺ SKBR-3 cell line and breast cancer tissues. Additionally, we compared fluorescence intensity (FI), photostability and staining index (SI) of QD525 signals at different exposure times and two excitation wavelengths with those of the conventional organic dye, FITC. Labeling signals of QD525 in both fixed and living breast cancer cells and tissue preparations were found to be significantly higher than those of FITC at 460–495 nm excitation wavelengths. Interestingly, when excited at 330–385 nm, the superiority of QD525 was more highlighted with at least 4–5 fold higher FI and SI compared to FITC. Moreover, QDs exhibited exceptional photostability during continuous illumination of cancerous cells and tissues, while FITC signal faded very quickly. QDs can be used as sensitive reporters for in situ detection of tumor markers which in turn could be viewed as a novel approach for early detection of cancers. To take comprehensive advantage of QDs, it is necessary that their optimal excitation wavelength is employed.     

The effect of zirconia content on properties of Al2O3–ZrO2 (Y2O3) composite nanopowders synthesized by aqueous sol–gel method

Al₂O₃–ZrO₂ (Y₂O₃) nanopowders containing 5, 10 and 15 wt% ZrO₂ were synthesized by aqueous sol–gel method using aluminum sec-butoxide and zirconium butoxide as precursors. BET analysis shows that, increasing the zirconia content results in a decrease in surface area, 152, 125 and 121 m²/g, and an increase in pore size, 5.63, 9.79 and 11.05 nm for 5, 10 and 15 wt% ZrO₂, respectively. Furthermore, a shift toward higher temperatures is observed for transition of transitional aluminas to stable α-alumina phase through increasing the zirconia content. SEM micrograph of calcined nanopowders revealed nanosize spherical particles in the range of 15–75 nm.     

Fracture assessment of polymethyl methacrylate using sharp notched disc bend specimens under mixed mode I + III loading

Mixed mode I/III behavior of Perspex (polymethyl methacrylate (PMMA)) is studied experimentally and theoretically in this research using a new and simple laboratory test configuration. The specimen is a circular disc containing a sharp V-notch along the diameter that is loaded by the conventional three-point bend fixture. The critical values of notch stress intensity factors (K _I ^V and K _III ^V ) were obtained for the whole combinations of modes I and III simply by changing the notch inclination angle relative to the loading rollers. The value of notch fracture toughness under pure or dominantly tension loads was greater than its corresponding value under mode III or dominantly torsion loads. The experimental results were also predicted very well by employing the local strain energy density (SED) criterion.     

Alum (KAl(SO4)2·12H2O) Catalyzed Multicomponent Transformation: Simple,Efficient, and Green Route to Synthesis of Functionalized Spiro[chromeno[2,3‐d]pyrimidine‐5,3′‐indoline]‐tetraones in Ionic Liquid Media

The combination of isatin, barbituric acid, and cyclohexane‐1,3‐dione derivatives in the presence of alum (KAl(SO₄)₂·12H₂O) as a catalyst for 15 min was found to be a suitable and efficient method for the synthesis of spiro[chromeno[2,3‐d]pyrimidine‐5,3′‐indoline]‐tetraones.     

Enhancing endothelial differentiation of human mesenchymal stem cells by culture on a nanofibrous polycaprolactone/(poly-glycerol sebacate)/gelatin scaffold

Cardiovascular diseases have always been one of the main causes of death worldwide and eventually one of the major medical concerns. Tissue engineering is promising strategies of treating cardiovascular, which can be an effective approach with the design of appropriate scaffold. In this study, to develop engineering basement membrane for endothelial differentiation with good cell attachment, we produced polycaprolactone (PCL)/poly (glycerol sebacate) (PGS)/gelatin nanofibrous scaffold via electrospinning. Attenuated total reflectance-Fourier transform infrared and the proton nuclear magnetic resonance results confirmed the chemical structure of synthesized PGS. Scanning electron microscope images of the electrospun scaffold revealed that the nanofibers are smooth, continues and uniform. Moreover, due to the presence of hydrophilic functional groups in the scaffold, the contact angle is in the appropriate range for cell adhesion especially endothelial cells. The elastic modulus and ultimate tensile stress of electrospun scaffold were calculated 1.32 ± 0.27 MPa and 1.23 ± 0.18 MPa respectively. Quantitative polymerase chain reaction was performed for evaluation of endothelial differentiation of mesenchymal stem cells cultured on standard plate and fibrous scaffold under chemical stimulation with growth factor. Specific endothelial gene expression results postulated that our modified scaffold could support and significantly promote endothelial differentiation of MSCs.