Search results for " Pharmaceutic"
showing 5 items of 865 documents
Synthesis and Biological Evaluation of a Multiantigenic Tn/TF-Containing Glycopeptide Mimic of the Tumor-Related MUC1 Glycoprotein
2006
Synthesis, antiproliferative activity, and in silico insights of new 3-benzoylamino-benzo[ b ]thiophene derivatives
2014
A new series of 3-benzoylamino-5-imidazol-5-yl-benzo[b]thiophenes and the parent amino derivatives were synthesized and screened as antitumor agents. All tested compounds showed concentration-dependent antiproliferative activity profile against HeLa cell line, exhibiting GI50 values in the low micromolar range. The most active compounds were tested in cell cycle perturbation experiments. A rapid accumulation of cells in the G2/M phase, with a concomitant reduction of cells in both the S and G0/G1 phases, was observed, suggesting that cell exposure to selected derivatives produces mitotic failure. To rationalize the biological results, the 3-benzoylamino-benzo[b]thiophenes were analyzed thro…
Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action
2015
Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsins B and L, and were found to be potent and selective inhibitors of rhodesain. Among them (S,E)-ethyl 5-((S)-2-{[(benzyloxy)carbonyl]amino}-3-phenylpropanamido)-7-methyl-4-oxooct-2-enoate (6) was the most potent, with an IC50 value of 16.4 nm and kinact/Ki=1.6×106 m−1 s−1 against rhodesain. These dipeptidyl enoates display a reversible mode of inhibition at very low concentrations and an irreversible mode at higher concentrations. Inhibition…
In-Depth Characterization of Bioactive Extracts from Posidonia oceanica Waste Biomass
2019
© 2019 by the authors.
Chemical Composition of the Essential Oil of Bupleurum Fontanesii (Apiaceae) Growing Wild in Sicily and its Activity on Microorganisms Affecting Hist…
2016
Hydrodistillation of the flowers (BpFl) of and fruits (BpFr) of Bupleurum fontanesii Guss. ex Caruel gave two oils that were analyzed by GC and GC-MS. The main components were α-elemol (16.7%), caryophyllene oxide (16.4%) and heptacosane (15.9%) in BpFl, and spathulenol (16.8%), caryophylladienol I (13.2%) and α-elemol (12.8%) in BpFr. A good antimicrobial activity against several microorganisms, including Bacillus subtilis, Staphylococcus aureus, Fusarium oxysporum and Aspergillus niger, all infesting historical art craft, was also determined.