Synthesis and biological evaluation of substituted pyrrolidines and pyrroles as potential anticancer agents.
Jiali JiFarrukh SajjadQun YouDong XingHui FanAlavala G K ReddyWenhao HuSuzhen DongPublished in: Archiv der Pharmazie (2020)
A series of polysubstituted pyrrolidines obtained via ruthenium-catalyzed cascade cyclization of diazo pyruvates and anilines as well as their corresponding pyrrole analogs obtained via dehydration were evaluated for their antiproliferation activities. Pyrrolidines 3h and 3k showed good proliferation inhibitory effects toward 10 cancer cell lines with IC50 values ranging from 2.9 to 16 μM. Furthermore, pyrrolidine 3k induced cell cycle arrest at the G0/G1 phase and time- and dose-dependent cellular apoptosis in both HCT116 and HL60 cells, suggesting that this type of pyrrolidine structure might be a good candidate for future anticancer therapies.
Keyphrases
- cell cycle arrest
- cell death
- pi k akt
- signaling pathway
- molecular docking
- papillary thyroid
- high glucose
- diabetic rats
- squamous cell
- current status
- room temperature
- cell proliferation
- drug induced
- oxidative stress
- young adults
- squamous cell carcinoma
- endothelial cells
- induced apoptosis
- ionic liquid
- endoplasmic reticulum stress