Synthesis and in vitro antitumor activity of 1-(3-dimethylamino)propyl indolin-2-one derivatives
Synthesis and in vitro antitumor activity of 1-(3-dimethylamino)propyl indolin-2-one derivatives
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DOI：
10.1007/s00044-012-0170-3
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发表时间：
2013-04-01
影响因子：
2.6
通讯作者：
Li, Song
中科院分区：
文献类型：
--
作者：
Lv, Kai;Wang, Li-Li;Li, Song
根据TMP-20、LK-B030和BX-517的结构特点，设计合成了一系列1-（3-二甲氨基丙基）吲哚啉-2- 1衍生物。这些新合成的衍生物对五种人类癌细胞系和三种HUVECs的体外活性进行了评估。结果显示，所有的靶化合物1a-h普遍对这些癌细胞系表现出有效的活性，并且对VEGF和bfgf刺激的HUVEC的选择性高于HUVEC。其中，1f （IC(50)s: 1.10 ~ 1.47 μ M）对MDA-MB-231、A549、HL-60、K-562的效价是舒尼替尼的1.8 ~ 6.0倍，对MDA-MB-231、A549的效价是LK-B030的1.6 ~ 2.8倍。
A series of 1-(3-dimethylaminopropyl)indolin-2-one derivatives were designed and synthesized based on the structural features of TMP-20, LK-B030, and BX-517. These newly synthesized derivatives were evaluated for in vitro activity against five human cancer cell lines and three HUVECs. Results revealed that all of the target compounds 1a-h generally show potent activity against these cancer cell lines and higher selectivity on VEGF- and bFGF-stimulated HUVECs than HUVEC. In particular, 1f (IC(50)s: 1.10-1.47 mu M) is 1.8-6.0-fold more potent than sunitinib against MDA-MB-231, A549, HL-60 and K-562, and 1.6-2.8-fold more potent than LK-B030 against MDA-MB-231 and A549.