1-苯胺基-5H-哒嗪并[4,5-b]吲哚类化合物的合成及体外抗肿瘤活性

目的设计并合成1-苯胺基-5H-哒嗪并[4,5-b]吲哚类化合物,评价其体外抗肿瘤活性。方法以5-乙酰氧基-6-溴-2-溴甲基-1-环丙基-1H-吲哚-3-羧酸乙酯为起始原料,经8～9步反应合成目标化合物;采用MTT法,测定了目标化合物对肿瘤细胞株Bel-7402和HT-1080的抑制活性。结果与结论合成了12个新化合物,其结构经1H-NMR和MS确证;多个化合物显示出良好的抗肿瘤活性,化合物10a和10d活性突出,对肿瘤细胞株Bel-7402和HT-1080的抑制活性分别是阳性对照药gefitinib的4倍和5倍,值得进一步研究。

Synthesis and antitumor activities of novel 1-anilino-5H-pyridazino[4,5-b]indoles

Aim To design and synthesize 1-anilino-5H-pyridazino[4,5-b]indole derivatives and evaluate their antitumor activities in vitro.Methods The target compounds were synthesized in 8-9 steps starting from ethyl 5-acetoxy-6-bromo-2-bromomethyl-1-cyclopropylindole-3-carboxylate and their antitumor activities against cancer cell lines Bel-7402 and HT-1080 were tested by MTT method.Results and conclusion Twelve new compounds were synthesized and their structures were confirmed by 1H-NMR and MS.Many compounds exhibited potent anticancer activity,while compounds 10a and 10d,whose IC50 values against Bel-7402 and HT-1080 was 4 and 5 times superior to the control gefitinib respectively,displayed promising activities and were worth further studying.