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Palmer, BD ; Henare, K ; Woon, ST ; Sutherland, R ; Reddy, C ; Wang, LCS ; Kieda, C ; Ching, LM

Synthesis and biological activity of azido analogues of 5,6-dimethylxanthenone-4-acetic acid for use in photoaffinity labeling

Journal of Medicinal Chemistry 50 3757-3764

par Administrateur - publié le

Abstract :

5,6-Dimethylxanthenone-4- acetic acid (1) is scheduled for phase III clinical trials as a vascular disrupting agent. However, its biochemical receptor(s) have yet to be identified. In this report, the synthesis of azido analogues of I that could be used for photoaffinity labeling of proteins as an approach toward identifying its molecular targets is described. While 5-azidoxantfienone-4-acetic acid (2) and 5-azido-6-methylxantheone-4-acetic acid (3) were found to have biological activities similar to that of 1, 6-azido-5-methylxanthenone-4-acetic acid (4) was unstable and could not be evaluated.