Application of wedelolactone analogue as novel topoisomerase I toxic agent

The invention discloses application of wedelolactone derivatives I-IV or pharmaceutically acceptable salts of the wedelolactone derivatives I-IV in a topoisomerase I inhibitor and tumor treatment. Wedelolactone derivatives I-IV have an excellent inhibition effect on topoisomerase I, the activity of...

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Hauptverfasser: CHEN YUEXI, CAI YUNRUI, JI SUHUI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses application of wedelolactone derivatives I-IV or pharmaceutically acceptable salts of the wedelolactone derivatives I-IV in a topoisomerase I inhibitor and tumor treatment. Wedelolactone derivatives I-IV have an excellent inhibition effect on topoisomerase I, the activity of a compound III is close to that of camptothecin, and the compound III is a Top1 toxic agent; the wedelolactone derivatives I-IV have very strong anti-tumor activity, and effectively inhibit proliferation of tumor cells. 本发明公开了一种蟛蜞菊内酯衍生物I-IV或其药学上可接受的盐在拓扑异构酶I抑制剂和治疗肿瘤中的应用。蟛蜞菊内酯衍生物I-IV对拓朴异构酶I有优秀的抑制作用,化合物III的活性接近喜树碱,是一类Top1毒剂;蟛蜞菊内酯衍生物I-IV具有很强的抗肿瘤活性,有效抑制肿瘤细胞的增值。