Abstract
Isoaurostatin A (IAS-A) isolated from Thermomonospora alba showed weak inhibition against topoisomerase (topo) I (IC 50 = 307 μM). To get more strong inhibition, derivatives of IAS-A were prepared and their structure–activity relationships against topo I and II were investigated. The addition of hydroxyl group on aromatic rings increased the activities, 3-(3,4,5-trihydroxybenzylidene)-5-hydroxy-3 H-benzofuran-2-one (IAS- 9) showed strong inhibition (IC 50 = 3 μM) against topo I. And also, the increasing of hydroxyl group increased growth inhibition against a variety of cancer cells, and IAS- 9 showed most potent inhibition. Unlike camptothecin and etoposide, IAS- 9 neither stabilized DNA–topo cleavable complex nor intercalated into DNA, and it inhibited topo I and II noncompetitively. The inhibitory activities also increased by opening of lactone ring in the molecule of IAS- 9.
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