【摘要】 肿瘤、癌症已是目前威胁人类健康的头号杀手,传统细胞毒类药物对人体健康组织伤害较大,新的、低毒的特异性药物开发备受关注。靛玉红类药物具有低细胞毒性和出色激酶抑制活性,从蛋白质的转录与合成阶段抑制肿瘤细胞增值,表现出优异的抗肿瘤活性,且可通过结构修饰用于多种疾病的治疗药物。本文系统总结了近十几年来靛玉红类化合物的合成方法及改进、生物活性与构效关系以及作为多种蛋白激酶(CDKs、GSK-3等)抑制剂的抑制效果。更多还原

【Abstract】 Tumor and cancer have become the number one killer threatening human health. Traditional cytotoxic drugs do great harm to human health tissues, and the development of new and low toxic specific drugs has attracted much attention. Indirubin has low cytotoxicity and excellent kinase inhibitory activity. It can inhibit the proliferation of tumor cells from the transcription and synthesis stage of protein, and has excellent antitumor activity. It can also be used in many kinds of disease treatment drugs through structural modification. The improvement of synthesis method of indirubin, the progress of research on biological activity and structure-activity relationship, and the inhibition effect as inhibitors of various protein kinases(CDKs, GSK-3, etc.) in recent ten years were reviewed.更多还原