Novel selective inhibitors for human topoisomerase I, BM2419-1 and -2 derived from saintopin |
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Authors: | Ishiyama D Futamata K Futamata M Kasuya O Kamo S Yamashita F Kanazawa S |
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Institution: | Drug Discovery Research Laboratories, Kaken Pharmaceutical CO., LTD., Shizuoka, Japan. |
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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. |
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