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首页> 外文期刊>Crystal growth & design >Exploring Solid Form Landscape of Anticancer Drug Dimethylaminomicheliolide Fumarate: Crystal Structures Analysis, Phase Transformation Behavior, and Physicochemical Properties Characterization
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Exploring Solid Form Landscape of Anticancer Drug Dimethylaminomicheliolide Fumarate: Crystal Structures Analysis, Phase Transformation Behavior, and Physicochemical Properties Characterization

机译:探索抗癌药物的固体形式景观二甲基氨基脲醇富马酸盐:晶体结构分析,相变行为和物理化学特性表征

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摘要

Brain tumors are still the deadliest among all types of cancer even after decades of extensive research. Glioblastoma is the most common and aggressive form of primary malignant brain tumors. As an efficient NF-kappa B inhibitor, dimethylaminomicheliolide fumarate has shown excellent therapeutic effect for glioblastoma in clinical trials. To date, no reports about the solid forms of dimethylaminomicheliolide fumarate have been disclosed. Dimethylaminomicheliolide fumarate was thus an interesting subject for polymorphism exploration. In this work, four solid forms (Forms B, C, D, and E) were successfully obtained. The crystal structures exhibit similarity in molecular conformation and packing arrangements between Form C and Form E. The PXRD patterns and phase transition behavior suggest that Form B and Form D are likely to have similarities. Hirshfeld surfaces were generated for a better understanding of the relationships of different crystal forms. They were also characterized and evaluated by thermal analysis, polarizing microscope, and dynamic vapor sorption as well as powder properties tests. The comprehensive exploration of the solid form landscape provided essential knowledge for product development and quality control of this potential drug.
机译:即使经过几十年的广泛研究,脑肿瘤仍然是所有类型癌症中最致命的。胶质母细胞瘤是原发性恶性脑肿瘤中最常见、最具侵袭性的一种。作为一种有效的NF-κB抑制剂,富马酸二甲氨基米其林在临床试验中对胶质母细胞瘤显示出良好的治疗效果。到目前为止,还没有关于富马酸二甲氨基二氯醚固体形式的报道。因此,富马酸二甲氨基米其林酯是多态性研究的一个有趣课题。在这项工作中,成功地获得了四种固体形态(形态B、C、D和E)。晶型C和晶型E之间的晶体结构在分子构象和排列上表现出相似性。PXRD模式和相变行为表明晶型B和晶型D可能具有相似性。为了更好地理解不同晶型之间的关系,制作了Hirshfeld表面。还通过热分析、偏光显微镜、动态蒸汽吸附以及粉末性能测试对其进行了表征和评估。对固体形态景观的全面探索为这种潜在药物的产品开发和质量控制提供了必要的知识。

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  • 来源
    《Crystal growth & design》 |2021年第5期|共10页
  • 作者单位

    Tianjin Univ State Key Lab Chem Engn Sch Chem Engn &

    Technol Tianjin 300072 Peoples R China;

    Tianjin Univ State Key Lab Chem Engn Sch Chem Engn &

    Technol Tianjin 300072 Peoples R China;

    Tianjin Univ State Key Lab Chem Engn Sch Chem Engn &

    Technol Tianjin 300072 Peoples R China;

    Tianjin Univ State Key Lab Chem Engn Sch Chem Engn &

    Technol Tianjin 300072 Peoples R China;

    Tianjin Univ State Key Lab Chem Engn Sch Chem Engn &

    Technol Tianjin 300072 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 晶体学;
  • 关键词

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