Synthesis of derivatives of methyl rosmarinate and their inhibitory activities against matrix metalloproteinase-1 (MMP-1)

  • Eur J Med Chem. 2013 Apr:62:148-57. doi: 10.1016/j.ejmech.2012.09.047.
Hu Yuan  1 ,  Weiqiang Lu ,  Liyan Wang ,  Lei Shan ,  Honglin Li ,  Jin Huang ,  Qingyan Sun ,  Weidong Zhang
Affiliations
  • 1. Department of Phytochemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
PMID: 23353736 DOI: 10.1016/j.ejmech.2012.09.047
Abstract

A series of MMP-1 inhibitors have been identified based upon a methyl rosmarinate scaffold using structure-based drug design methods. The best compound in the series showed an IC50 value of 0.4 μM. A docking study was conducted for compound (S)-10n in order to investigate its binding interactions with MMP-1. The structure-activity relationships (SAR) were also briefly discussed. Useful SAR was established which provides important guidelines for the design of future generations of potent inhibitors against MMP-1.

Products