Fluorinated and N-Acryloyl-Modified 3,5-Di[(E)-benzylidene]piperidin-4-one Curcuminoids for the Treatment of Pancreatic Carcinoma
نویسندگان
چکیده
Pancreatic carcinoma is a cancer disease with high mortality. Thus, new and efficient treatments for this are badly needed. Curcumin has previously shown promising effects in pancreatic patients; however, natural compound suffers from inadequate efficacy bioavailability, preventing its clinical approval. The synthetic curcuminoid EF24 was developed activities superior to curcumin against various types. In study, series of analogs were investigated anticancer on models. A distinct activity boost achieved by straightforward N-acrylation analogs, particular, compounds bearing 3-fluoro-4-methoxybenzylidene, 3,4-difluorobenzylidene, 4-trifluoromethylbenzylidene moieties, while no improvement seen N-acryloyl-modified EF24. Apoptosis induction suppression phospho-STAT3 levels determined, the latter corroborated docking active curcuminoids into STAT3. Hence, clues development as valuable treatment options one most lethal diseases discovered study.
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ژورنال
عنوان ژورنال: Pharmaceutics
سال: 2023
ISSN: ['1999-4923']
DOI: https://doi.org/10.3390/pharmaceutics15071921