Methyl isoindigo derivative as well as preparation method and application thereof
The invention discloses a methylisoindigo derivative as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The invention provides a methylisoindigo derivative (methylisoindigo PROTAC molecule), a pharmaceutical composition taking the meth...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses a methylisoindigo derivative as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The invention provides a methylisoindigo derivative (methylisoindigo PROTAC molecule), a pharmaceutical composition taking the methylisoindigo derivative as an active ingredient, and application of the methylisoindigo derivative in preparation of an ATM degradation agent, and further provides application of the methylisoindigo derivative in preparation of an antitumor drug, the methylisoindigo derivative degrades ATM, inhibits DNA double-chain damage repair and blocks a cell cycle in a G0/G1 phase, so that cell apoptosis is induced, and the antitumor effect of the methylisoindigo derivative is improved. The anti-tumor effect is achieved.
本发明公开了一种甲异靛衍生物及其制备方法与应用,属于药物化学技术领域;本发明提供了一种甲异靛衍生物(甲异靛PROTAC分子),以其为活性成分的药物组合物,以及在制备ATM降解剂中的应用,还提供了甲异靛衍生物在制备抗肿瘤药物中的应用,该衍生物通过降解ATM,抑制DNA双链损伤修复,将细胞周期阻滞在G0/G1期,从而诱导细胞凋亡,发挥抗肿瘤作用。 |
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