Synthesis of a cyclic analogue of galardin

Authors
Ma, DW Wu, WG Qian, J Lang, SH Ye, QZ
Citation
Dw. Ma et al., Synthesis of a cyclic analogue of galardin, CHIN J CHEM, 19(3), 2001, pp. 286-290
Citations number
10
Categorie Soggetti
Chemistry
Journal title
CHINESE JOURNAL OF CHEMISTRY
ISSN journal
1001604X → ACNP
Volume
19
Issue
3
Year of publication
2001
Pages
286 - 290
Database
ISI
SICI code
1001-604X(200103)19:3<286:SOACAO>2.0.ZU;2-5
Abstract
A cyclic analogue 4 of galardin, a known MMP inhibitor, is designed to impr ove its selectivity. The synthesis of 4 starts from dimethyl (S)-malate usi ng diaselective alkylation and subsequent cyclization and amide formation a s key steps. The compound 4 showed MMP inhibitory activity on all MMPs test ed with IC50 ranging from 20.1 muM to 104 muM.