Design, synthesis and potent anti-pancreatic cancer activity of new pyrazole derivatives bearing chalcone, thiazole and thiadiazole moieties: gene expression, DNA fragmentation, cell cycle arrest and SAR.

ABSTRACT: Less than 5% of pancreatic cancer patients survive for more than five years after diagnosis. Therefore, there is an urgent need for novel therapeutic drugs to treat pancreatic cancer. Herein, we report the synthesis and full characterization of fifteen novel pyrazole derivatives bearing chalcone (4-10), thiazole (16-19) and thiadiazole (23-26) moieties. All the newly synthesized pyrazole derivatives were tested in vitro as anti-cancer agents against pancreatic cancer (PaCa-2), breast cancer (MCF-7), prostate cancer (PC3), and normal cell lines (BJ1). Three pyrazolyl-chalcone derivatives (4, 5, and 7) and a pyrazolyl-thiadiazole derivative (25) showed potent anti-cancer activity against the PaCa-2 cell line with IC₅₀ values of 13.0, 31.5, 24.9, and 5.5 μg mL^-1,

SUBMITTER: Kamel MG 

PROVIDER: S-EPMC11348842 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature