| 18528783 |
Baqi Y, Weyler S, Iqbal J, Zimmermann H, Muller CE: Structure-activity relationships of anthraquinone derivatives derived from bromaminic acid as inhibitors of ectonucleoside triphosphate diphosphohydrolases (E-NTPDases). Purinergic Signal. 2009 Mar;5(1):91-106. Epub 2008 Jun 5.
The 2-sulfonate group was found to be required for inhibitory activity, since 2-methyl-substituted derivatives were inactive. 1-Amino-2-sulfo-4-p-chloroanilinoanthraquinone (18) was identified as a nonselective competitive blocker of NTPDases1, 2, and 3 (K (i) 16-18 muM), while 1-amino-2-sulfo-4-(2-naphthylamino) anthraquinone (21) was a potent inhibitor with preference for NTPDase1 (K (i) 0.328 muM) and NTPDase3 (K (i) 2.22 muM). |
164(2,2,2,4) |
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