Design, Synthesis, and Antipoliferative Activities of Novel Substituted Imidazole-Thione Linked Benzotriazole Derivatives

A new series of benzotriazole moiety bearing substituted imidazol-2-thiones at N1 has been designed, synthesized and evaluated for in vitro anticancer activity against the different cancer cell lines MCF-7(breast cancer), HL-60 (Human promyelocytic leukemia), and HCT-116 (colon cancer). Most of the benzotriazole analogues exhibited promising antiproliferative activity against tested cancer cell lines. Among all the synthesized compounds, BI9 showed potent activity against the cancer cell lines such as MCF-7, HL-60 and HCT-116 with IC50 3.57, 0.40 and 2.63 µM, respectively. Compound BI9 was taken up for elaborate biological studies and the HL-60 cells in the cell cycle were arrested in G2/M phase. Compound BI9 showed remarkable inhibition of tubulin polymerization with the colchicine binding site of tubulin. In addition, compound BI9 promoted apoptosis by regulating the expression of pro-apoptotic protein BAX and anti-apoptotic proteins Bcl-2. These results provide guidance for further rational development of potent tubulin polymerization inhibitors for the treatment of cancer.

Preparation and preliminary quality evaluation of aspirin/L-glutamate compound pellets

L-glutamate is an important component of protein. It can prevent gastrointestinal damage caused by NSAIDs. We constructed two-phase enteric-coated granules of aspirin and L-glutamate compound by extrusion spheronization method and fluidized bed coating. The subliminal effective dose of L-glutamate is 100 mg/kg tested by model of gastric ulcer of rats induced by aspirin and drug administration. HPLC-UV and UV–Vis methods were adopted to determine content and cumulative release of aspirin and L-glutamate as quality analysis method indexes. The prescription and process optimization were carried out with yield, sphericity and dissolution. The two-phase compound granules have good sphericity of 0.93 ± 0.05 (aspirin pellets) and 0.94 ± 0.02 (L-glutamate pellets), content of salicylic acid (0.24 ± 0.03)%, dissolution of aspirin (2.36 ± 0.11)%. Quality evaluation and preliminary stability meet the commercial requirements. The stored environment of compound preparation should be sealed in a cool and dark place.

Anti-Liver and Anti-Breast Cancer Activities of Novel 2-Thioxo-4-Imidazolidinone Derivatives

MTT assay and flowcytometry analysis were used to examine the anti-liver (HepG2) and anti-breast cancer (MCF-7) activities of twelve compounds derived from 2-thioxo-4-imidazolidine. The compounds 5a-h and 7f demonstrated significant anticancer activity against breast cancer cells, while the compounds 5a, ab, and 5d-h demonstrated significant anticancer activity against liver cancer cells, with varying IC50 values as compared to Cisplatin as the positive control. Among these compounds, we chose 5a, 5d, and 5h to detect cell cycle phases and late apoptosis. Compound 5a arrested MCF-7 cells in the S phase, while compound 5d arrested cells in the G1 phase. Compound 5a arrested S phase HepG2 cells, compound 5d arrested S phase cells, and compound 5h arrested G2 phase HepG2 cells. Compound 5a had a higher ratio of late apoptosis than compounds 5d and 5h on both cancer cells. Finally, the development of these compounds as new anti-breast and anti-liver agents warrants further research to understand the mechanism of action, especially against breast cancer.

Synthesis, Crystal Structure, and Ionic Conductivity of MgAl2-xGaxCl8 and MgGa2Cl7Br

MgAl2-xGaxCl8 and MgGa2Cl7Br was synthesized from MgCl2, MgBr2, AlCl3, and GaCl3, and the physical properties were evaluated by XRD, AC conductivity, and X-ray fluorescence. MgAl2-xGaxCl8 has the same crystal structure as MgAl2Cl8, belongs to the space group C2/c, and forms a solid solution in all the synthesized compositions. We attempted to MgGa2Cl8-yBry synthesize in the same manner as MgAl2Cl8, but only obtained MgGa2Cl7Br as a single-phase compound. The AC conductivity of MgAl2-xGaxCl8 was lowest for MgAl2Cl8 and highest for MgGa2Cl8. The conductivity of MgGa2Cl8 at 400 K was 1.7 × 10−6 S/cm. The conductivity of MgGa2Cl7Br was higher than that of MgAl2-xGaxCl8 with a value of 1.6 × 10−5 S/cm at 400 K. The formation of Mg metal was observed at the surface of the cathode electrode in an experiment of flowing a direct current using an electrochemical cell, indicating that this compound is a magnesium ion conductor.

Operando Calorimetry Informs the Origin of Rapid Rate Performance in Microwave-Prepared TiNb2O7 Electrodes

<div>The shear-phase compound TiNb₂O₇ has recently emerged as a safe and high-volumetric density replacement for graphite anodes in lithium ion batteries. An appealing feature of TiNb₂O₇ is that it retains capacity even at high cycling rates. Here we demonstrate that phase pure and crystalline TiNb₂O₇ can be rapidly prepared using a high-temperature microwave synthesis method. Studies of the charging and discharging of this material, including through operando calorimetry, permit key thermodynamic parameters to be revealed. The nature of heat generation is dominated by Joule heating, which sensitively changes as the conductivity of the electrode increases with increasing lithiation. The enthalpy of mixing, obtained from operando calorimetry, is found to be small across the different degrees of lithiation pointing to the high rate of lithium ion diffusion at the origin of rapid rate performance.</div>

Operando Calorimetry Informs the Origin of Rapid Rate Performance in Microwave-Prepared TiNb2O7 Electrodes

<div>The shear-phase compound TiNb₂O₇ has recently emerged as a safe and high-volumetric density replacement for graphite anodes in lithium ion batteries. An appealing feature of TiNb₂O₇ is that it retains capacity even at high cycling rates. Here we demonstrate that phase pure and crystalline TiNb₂O₇ can be rapidly prepared using a high-temperature microwave synthesis method. Studies of the charging and discharging of this material, including through operando calorimetry, permit key thermodynamic parameters to be revealed. The nature of heat generation is dominated by Joule heating, which sensitively changes as the conductivity of the electrode increases with increasing lithiation. The enthalpy of mixing, obtained from operando calorimetry, is found to be small across the different degrees of lithiation pointing to the high rate of lithium ion diffusion at the origin of rapid rate performance.</div>