Publications by authors named "Jian-Mei Qin"
A series of inhibitors of 20S proteasome based on terminal functionalized dipeptide derivatives containing the thiourea moiety were synthesized and evaluated for inhibition of 20S proteasome and the effects of multidrug-resistance reversers. These compounds exhibited significant selectivity to the β5-subunit of the human 20S proteasome with IC values at submicromolar concentrations. A docking study of the most active compound 6i revealed key interactions between 6i and the active site of the 20S proteasome in which the thiourea moiety and a nitro group were important for improving activity.
View Article and Find Full Text PDF4-Methylumbelliferones Analogues as Anticancer Agents: Synthesis and in Cell Pharmacological Studies.
Anticancer Agents Med Chem
August 2017
Article Synopsis
- Cancer remains a serious global health challenge, prompting research into new therapeutic agents, particularly natural and synthetic coumarin derivatives known for their diverse structures and biological activities.
- This study focused on synthesizing 4-MU derivatives with urea-piperazine and thioureapiperazine groups and tested their effectiveness as antitumor drugs against NCI-H460 cancer cells using various experimental methods.
- The key finding was that compound 4l showed strong anticancer properties by inducing apoptosis and cell cycle arrest in NCI-H460 cells, suggesting that it could be a promising candidate for further cancer treatment development.