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Synthesis of a Cyclic Analogue of Galardin |
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| Authors: | Da‐Wei Ma Wen‐Gen Wu Jing Qian Shen‐Hui Lang Qi‐Zhuang Ye |
| Abstract: | A cyclic analogue 4 of galardin, a known MMP inhibitor, is designed to improve its selectivity. The synthesis of 4 starts from dimethyl (S)‐malate using diaselective alkylation and subsequent cyclization and amide formation as key steps. The compound 4 showed MMP inhibitory activity on all MMPs tested with IC30, ranging from 20.1 μM to 104 μM. |
| Keywords: | Matrix metalloproteinases inhibitor alkylation cyclization amide |