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OALib Journal期刊
ISSN: 2333-9721
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吲哚咔唑类化合物及其衍生物的抗肿瘤活性
, PP. 368-374
Keywords: 吲哚咔唑,拓扑异构酶,蛋白激酶,DNA-拓扑异构酶I复合物,cyclin-CDK复合物,构效关系
Abstract:
吲哚咔唑类化合物是一类提取自微生物发酵液中的生物碱.这一类化合物及其衍生物如staurosporine、ED-110、NB-506、rebeccamycin、氮杂吲哚咔唑、吲哚咔唑糖缀合物、双吲哚马来酰亚胺等，被认为存在广泛的抗肿瘤作用靶点，包括多种与细胞周期有关的激酶、细胞核拓扑异构酶、与肿瘤细胞生长或凋亡相关的酶等。现已知，吲哚咔唑化合物是拓扑异构酶的致毒剂，其对蛋白激酶的抑制作用表现为竞争结合其ATP口袋上特异的氨基酸基团，从而抑制酶的活性，并引起细胞生长静止于G1期。多年来研究者们努力寻找此类化合物的良好结构，以期得到抗肿瘤活性提高的选择性激酶抑制剂。本文综述了吲哚咔唑类化合物的研究进展、临床应用、抗肿瘤活性产生的机制以及化合物的构效关系（SAR）等。
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