J Enzyme Inhib Med Chem
December 2023
A new series of bis-triazole was synthesised for the purpose of being hybrid molecules with both anti-inflammatory and anti-cancer activities and assessed for cell cycle arrest, NO release. Compounds , , , exhibited COX-2 selectivity indexes in the range of 18.48 to 49.
View Article and Find Full Text PDFTwo new series of pyrazolyl-thiazolidinone/thiazole derivatives and were synthesised, merging the scaffolds of celecoxib and dasatinib. Compounds , and inhibit with S.I.
View Article and Find Full Text PDFNew chromene derivatives were synthesized based on 4-(3,4-dimethoxy)-4H-chromene scaffold. All target compounds exhibited cytotoxic activity against HepG2 cells (IC = 2.40-141.
View Article and Find Full Text PDFDual inhibition of topoisomerase (topo) II and FLT3 kinase, as in the case of C-1311, was shown to overcome the shortcomings of using topo II inhibitors solely. In the present study, we designed and synthesized two series of pyrido-dipyrimidine- and pseudo-pyrido-acridone-containing compounds. The two series were evaluated against topo II and FLT3 as well as the HL-60 promyelocytic leukemia cell line in vitro.
View Article and Find Full Text PDFIn this study, three novel sets of 4-aryl-4H-chromene derivatives 4a-c, 6a-d and 7a-c were synthesized and evaluated for anticancer activity. Characterization of new compounds was established on basis of elemental analyses and spectral data. All new compounds were investigated for their antiproliferative activity against HCT-116, HepG-2 and MCF-7 cell lines using vinblastine and staurosporine as positive controls.
View Article and Find Full Text PDFAims: Unlike other Toll-like receptors (TLRs), the role of toll like receptor 2 (TLR-2) in the pathogenesis of chronic liver disease and hepatocellular carcinoma (HCC) is not well studied. We, therefore, set out to investigate the expression of TLR-2 in different chronic liver disease states along with other markers of cell death, cellular proliferation and tissue vascularisation METHODS AND RESULTS: Immunohistochemistry was performed on liver tissue microarrays comprising hepatitis, cirrhosis and HCC patient samples using antibodies against TLR-2, Ki-67, Caspase-3 and VEGF. This was done in order to characterise receptor expression and translocation, apoptosis, cell proliferation and vascularisation.
View Article and Find Full Text PDFThe original version of this article unfortunately contained an error. The Tables 1 and 2 were missing in the published paper.
View Article and Find Full Text PDFCaveolin-1, the major protein component of caveolae, plays vital functions in tumorigenesis and metastasis. Previous evidence demonstrated the positive role of Caveolin-1 in the regulation of endothelial cell differentiation and the involvement of Caveolin-1 in vascular endothelial growth factor (VEGF) mediated angiogenesis. The correlation of Caveolin-1 expression and angiogenesis is not yet elucidated in osteosarcoma.
View Article and Find Full Text PDF