: The role of transforming growth factor-beta1 (TGF-β1) has been widely studied in the context of carcinogenesis. It has been involved in the pathogenesis of primary brain tumors or brain metastases due to its pleiotropic effects on immune regulation and tissue homeostasis. In line with recent findings, the aim of the current study was to examine the role of circulating TGF-β1 and the -509C/T functional polymorphism (rs1800469) in the gene promoter in the susceptibility and progression of primary brain tumors and brain metastases among patients from the Bulgarian population.
View Article and Find Full Text PDFAlzheimer's disease (AD) is considered a complex neurodegenerative condition which warrants the development of multitargeted drugs to tackle the key pathogenetic mechanisms of the disease. In this study, two novel series of melatonin- and donepezil-based hybrid molecules with hydrazone () or sulfonyl hydrazone () fragments were designed, synthesized, and evaluated as multifunctional ligands against AD-related neurodegenerative mechanisms. Two lead compounds ( and ) exhibited a well-balanced multifunctional profile, demonstrating intriguing acetylcholinesterase (AChE) inhibition, promising antioxidant activity assessed by DPPH, ABTS, and FRAP methods, as well as the inhibition of lipid peroxidation in the linoleic acid system.
View Article and Find Full Text PDFBACKGROUND Gastrointestinal tract melanomas are usually of metastatic origin, with primary melanomas being relatively rare. Controversy arises about the existence of primary melanoma in the gastrointestinal tract except in areas where melanocytes exist. The appearance of primary colon melanoma is rare due to the embryological absence of melanocytes in the large intestine, with some authors denying its existence at all.
View Article and Find Full Text PDFBreast cancer (BC) is the second leading cause of cancer death in women, with more than 600,000 deaths annually. Despite the progress that has been made in early diagnosis and treatment of this disease, there is still a significant need for more effective drugs with fewer side effects. In the present study, we derive QSAR models with good predictive ability based on data from the literature and reveal the relationships between the chemical structures of a set of arylsulfonylhydrazones and their anticancer activity on human ER+ breast adenocarcinoma and triple-negative breast (TNBC) adenocarcinoma.
View Article and Find Full Text PDFFifteen 4-methyl-1,2,3-thiadiazole-based hydrazone derivatives - and sulfonyl hydrazones - were synthesized. They were characterized by H-NMR, C NMR, and HRMS. strain H37Rv was used to assess their antimycobacterial activity.
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