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Synthesis of a Cyclic Analogue of Galardin
Author(s) -
Ma DaWei,
Wu WenGen,
Qian Jing,
Lang ShenHui,
Ye QiZhuang
Publication year - 2001
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.20010190315
Subject(s) - chemistry , alkylation , selectivity , amide , stereochemistry , cyclic peptide , combinatorial chemistry , organic chemistry , biochemistry , peptide , catalysis
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 IC 30 , ranging from 20.1 μM to 104 μM.
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