Beijing Institute of Radiation Medicine, Beijing 100850, China.
Molecules. 2017 Nov 16;22(11):1979. doi: 10.3390/molecules22111979.
In this work, a series of novel benzyl sulfoxide 2-indolinone derivatives was designed and synthesized as potent anticancer agents. Tyrosine kinase inhibitory activity assay indicated that most of the compounds showed significant activity. The in vitro antiproliferative activity of these compounds was further investigated against five human cancer cell lines (HeLa, HepG2, MCF-7, SCC-15, and A549). Several compounds exhibited evident activities. Among them, ()-3-(((4-bromobenzyl)sulfinyl)methylene)indolin-2-one () and ()-3-((benzylsulfinyl)methylene)-5-bromoindolin-2-one () were found to be effective tyrosine kinase inhibitors (IC = 1.34 and 2.69 μM, respectively) in addition to having noteworthy antitumor potential (the average IC value of or was less than 40 μM). This class of novel derivatives has promising potential for further development as anticancer agents.
在这项工作中，设计并合成了一系列新型的苄基砜 2-吲哚啉酮衍生物，作为有效的抗肿瘤药物。酪氨酸激酶抑制活性测定表明，大多数化合物表现出显著的活性。进一步研究了这些化合物对五种人癌细胞系（HeLa、HepG2、MCF-7、SCC-15 和 A549）的体外增殖活性。一些化合物表现出明显的活性。其中，（）-3-(((4-溴苄基)亚砜基)亚甲基)吲哚啉-2-酮（）和（）-3-((苄基亚砜基)亚甲基)-5-溴吲哚啉-2-酮（）被发现是有效的酪氨酸激酶抑制剂（IC = 1.34 和 2.69 μM），同时具有显著的抗肿瘤潜力（或的平均 IC 值均小于 40 μM）。这一类新型衍生物具有作为抗肿瘤药物进一步开发的潜力。
