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A new short synthesis of 5,6-dimethylxanthenone-4-acetic acid (ASA404, DMXAA)

✍ Scribed by Shangjin Yang; William A. Denny


Publisher
Elsevier Science
Year
2009
Tongue
French
Weight
217 KB
Volume
50
Category
Article
ISSN
0040-4039

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✦ Synopsis


A new short synthesis of 5,6-dimethylxanthenone-4-acetic acid (ASA404) is developed. The key steps of the synthesis are dibromination of 3,4-dimethylbenzoic acid, followed by regioselective coupling with 2hydroxyphenylacetic acid and subsequent cyclodehydration.


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## Abstract The novel vascular targeting agent 5,6‐dimethylxanthenone‐4‐acetic acid (DMXAA) has completed phase 1 clinical trial and has shown tumor antivascular activity in both mice and humans. We have investigated its ability to change tumor vascular permeability, relating it to tumor vascular p