Novel Selective Inhibitors for Human Topoisomerase I, BM2419-1 and -2 Derived from Saintopin

Abstract

Compounds BM2419-1 and -2 were isolated from a culture broth of a fungus Paecilomyces sp. BM2419. It was shown that these novel compounds were artifacts derived from saintopin, a dual inhibitor of topoisomerase I and II by independent processes. In the human topoisomerase I inhibition assay using the recombinant Saccharomyces cerevisiae, BM2419-1 and -2 inhibited selectively the yeast growth dependent on human topoisomerase I induction with IC₅₀ values of 0.3 ng/ml and 6.0 ng/ml, respectively.