小分子DNA嵌插剂的最新研究进展

发布时间：2019-08-03 20:50

【摘要】：DNA嵌插剂是一类能与DNA相互作用并与之形成嵌插复合物的多环小分子化合物,在癌症化疗中前景广阔。通过嵌插结合,DNA嵌插剂可以直接抑制DNA的复制与转录,或经过进一步活化裂解DNA进而影响其结构和功能。设计新高效的DNA嵌插剂是一种可以推进临床癌症化疗的可行性方法,已有多个DNA嵌插剂开发用于白血病等肿瘤的治疗。近年新合成的具有代表性的DNA嵌插剂主要有喹啉和喹唑啉骨架衍生物、吩嗪骨架衍生物、吲哚骨架衍生物、吖啶骨架衍生物、异恶唑烷基多环芳烃衍生物、螺纹嵌插剂以及其他骨架嵌插剂等。嵌插剂所具有的嵌插结合性质使其除了可以用作以DNA为靶点的多种肿瘤的直接治疗外,还可以作为DNA结构的诊断探针。
[Abstract]:DNA intercalation agent is a kind of polycyclic small molecule compound which can interact with DNA and form intercalation complex with it. It has a broad prospect in cancer chemotherapy. Through intercalation binding, DNA intercalation agent can directly inhibit the replication and transcription of DNA, or further activate and cleave DNA and then affect its structure and function. The design of new and efficient DNA intercalation agent is a feasible method to promote clinical cancer chemotherapy. A number of DNA inserts have been developed for the treatment of leukemia and other tumors. In recent years, the main representative DNA intercalators are quinolin and quinazolin skeleton derivatives, phenazine skeleton derivatives, indole skeleton derivatives, acridine skeleton derivatives, isooxazole alkyl polycyclic aromatic hydrocarbons derivatives, thread intercalators and other skeleton intercalators, etc., which are mainly composed of quinolin and quinazolin skeleton derivatives, indole skeleton derivatives, acridine skeleton derivatives, isoxazole alkyl polycyclic aromatic hydrocarbons derivatives, thread inserts and other skeleton intercalators. Because of its intercalation binding properties, the intercalation agent can not only be used as a direct treatment for a variety of tumors targeting DNA, but also as a diagnostic probe for the structure of DNA.
【作者单位】：青岛大学附属医院;中国科学院海洋研究所·实验海洋生物学重点实验室·中国科学院大学;
【基金】：国家自然科学基金资助项目(41506169)
【分类号】：R979.1

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