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Ⅱ—7是经对中药“当归芦荟丸”抗癌有效成分靛玉红结构改造而来,具有较高抗肿瘤活性和较低的毒性。本组以Ⅱ—7为母体合成了一系列衍生物,这是抗肿瘤药物中一类结构全新的化合物,其抗肿瘤活性,国内外文献均未见报道。该化合物全部进行了体外细胞毒试验,选用L_(1210)细胞株得到了抑制50%细胞生长的浓度IC_(50),并以log1/I C_(50)作为生物活性指标与化合物理化参数建立了QS AR方程: log1/IC_(50)=6.3200-0.159(±0.082)logP-
Ⅱ-7 is the Chinese medicine “Angelica aloe pill” anti-cancer active ingredients from the structure of indirubin transformed from high anti-tumor activity and low toxicity. This group of Ⅱ-7 as a precursor to the synthesis of a series of derivatives, which is a class of anti-tumor drugs with a new structure, its anti-tumor activity, domestic and foreign literature have not been reported. All of the compounds were tested in vitro cytotoxicity. The IC50 of 50% cell growth was determined by using L1210 cell line and the log1 / I C50 (50) was used as bioactivity index to establish the physical and chemical parameters of the compound QS AR equation: log1 / IC_ (50) = 6.3200-0.159 (± 0.082) logP-