Abstract:In this study, novel aminothiazole-paeonol derivatives were synthesized and characterized using 1 H-NMR, 13 C-NMR, IR, mass spectroscopy, and high performance liquid chromatography. All the new synthesized compounds were evaluated according to their anticancer effect on seven cancer cell lines. The experimental results indicated that these compounds possess high anticancer potential regarding human gastric adenocarcinoma (AGS cells) and human colorectal adenocarcinoma (HT-29 cells). Among these compounds, N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]-4-methoxybenzenesulfonamide (13c) had the most potent inhibitory activity, with IC 50 values of 4.0 µM to AGS, 4.4 µM to HT-29 cells and 5.8 µM to HeLa cells. The 4-fluoro-N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]benzenesulfonamide (13d) was the second potent compound, showing IC 50 values of 7.2, 11.2 and 13.8 µM to AGS , HT-29 and HeLa cells, respectively. These compounds are superior to 5-fluorouracil (5-FU) for relatively higher potency against AGS and HT-29 human cancer cell lines along with lower cytotoxicity to fibroblasts. Novel aminothiazole-paeonol derivatives in this work might be a series of promising lead compounds to develop anticancer agents for treating gastrointestinal adenocarcinoma.
Highlights
Differential splicing profiles of
MBNL1
and
Acin1
gene is noted in CRC tissues or cells.
Autoregulated exclusion of
MBNL1
exons is altered with upregulated SRSF3
MBNL1 isoform differentially modulates CRC-related AS events.
SRSF3 and MBNL1 exerts opposite impact on expression of the Acin1 isoform.
Acin1 isoform exhibits distinct influence on DNA fragmentation in CRC cells.
SRSF3-MBNL11-Acin1 constitutes an emerging circuit involved in apoptosis of CRC cells.
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