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目的合成一类新型的N,N-二取代苯乙胺衍生物并研究其体外抗肿瘤活性。方法以N-Boc哌啶酮为起始原料,经过还原胺化、N-酰化、N-Boc保护基脱除等反应得到目标化合物;采用MTT法在小鼠黑色素瘤B16、人肺癌A549、人结直肠癌HCT116、人恶性黑色素瘤A375等细胞株上测试其体外抗肿瘤活性。结果与结论合成了7个新型化合物,并经1HNMR、MS确证了化学结构。初步的体外抗肿瘤活性显示:化合物Ⅲb具有良好的抗黑色素瘤活性及选择性。
Objective To synthesize a new class of N, N-disubstituted phenylethylamine derivatives and study their anti-tumor activity in vitro. Methods N-Boc piperidone was used as a starting material to get the target compound through reductive amination, N-acylation and N-Boc deprotection. The target compounds were obtained by MTT assay in mouse melanoma B16, human lung adenocarcinoma A549, Human colorectal cancer HCT116, human malignant melanoma A375 and other cell lines tested its anti-tumor activity in vitro. RESULTS AND CONCLUSIONS Seven novel compounds were synthesized and confirmed by 1H NMR and MS. Preliminary in vitro antitumor activity showed that compound IIIb had good anti-melanoma activity and selectivity.