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The present study was planned to design some novel aldimine‐type Schiff bases bearing 3,4,5‐trimethoxyphenyl and 1,2,4‐triazole‐3‐thione/thiol as potential tubulin polymerization inhibitors. The obtained results of the molecular docking study using the tubulin complex (PDB code: 1SA0) showed that compounds H‐25 and H‐26 were well fitted in the colchicine binding site of tubulin with binding energies of −8.68 and −8.40 kcal/mol, respectively, in comparison to the main ligand (−8.20 kcal/mol). In parallel, molecular simulations were also performed on five other 3,4,5‐trimethoxyphenyl‐containing ligand targets including hsp90, VEGFR2, and human and microbial (Staphylococcus aureus and Candida albicans) dihydrofolate reductase, among which H‐17, H‐45, H‐27, H‐02, and H‐19 were the most suitable compounds, respectively. Evaluation of the cytotoxic effect of the most efficient compounds of the docking steps (H‐25) revealed IC50 values of 12.48 ± 1.10, 4.25 ± 0.22, 3.33 ± 0.31, and 9.71 ± 0.75 µM against the HT1080, HT29, MCF‐7, and A549 cell lines, respectively, compared to doxorubicin (12.69 ± 1.23, 6.12 ± 0.47, 3.51 ± 0.32, and 6.40 ± 0.31 µM, respectively). The in vitro tubulin polymerization investigation launched compounds H‐25 and H‐26 as potent antitubulin agents due to their IC50 values of 0.17 ± 0.01 and 10.93 ± 0.43 µM, respectively.
A series of hybrid aldimine‐type Schiff base derivatives consisting of a trimethoxyphenyl ring and 1,2,4‐triazole‐3‐thione/thiol were designed and their cytotoxic activities and anti‐tubulin effects were investigated. The molecular docking study on the tubulin complex (PDB code: 1SA0), in vitro tubulin polymerization assays and MTT assays on five human cancer cell lines revealed H‐25 as the most active compound.
Abstract The single radial immunodiffusion assay has been the accepted method for determining the potency of inactivated influenza vaccines since 1978. The world‐wide adoption of this assay for vaccine standardisation was facilitated through collaborative studies that demonstrated a high ... mehr
Abstract Background Whether morbidity from the 1918‐19 influenza pandemic discriminated by socioeconomic status has remained a subject of debate for 100 years. In lack of data to study this issue recent literature have hypothesized that morbidity was “socially neutral”. Objectives ... mehr