Design, synthesis and preliminary evaluation of new cinnamoyl pyrrolidine derivatives as potent gelatinase inhibitors.

@article{Zhang2006DesignSA,
  title={Design, synthesis and preliminary evaluation of new cinnamoyl pyrrolidine derivatives as potent gelatinase inhibitors.},
  author={Li Zhang and Jie Zhang and Hao Fang and Qiang Wang and Wenfang Xu},
  journal={Bioorganic & medicinal chemistry},
  year={2006},
  volume={14 24},
  pages={8286-94}
}
A series of new cinnamoyl pyrrolidine derivatives have been synthesized based on the l-hydroxyproline scaffold and inhibiting activities on gelatinase (MMP-2 and -9) and APN were tested. Structure-activity relationship studies showed that the side chain with aromatic ring at C4 in pyrrolidine ring showed better inhibitory activities on gelatinase than aliphatic side chain. Most compounds exhibited poor activities on APN compared with MMP-2. Within this series, three compounds, A8, B9 and C10… CONTINUE READING