1,2-苯并噻嗪类化合物的合成及抗肿瘤活性研究

Synthesis and antitumor activity evaluation of 1,2-benzothiazine derivatives

根据拼合原理,设计合成了一系列全新的具有拉帕替尼和诺拉替尼分子片段的1,2-苯并噻嗪类化合物,其结构均经IR、1H NMR、13C NMR和MS确证。考察所合成化合物的体外抗肿瘤细胞(A549,MCF-7)活性,结果表明,所合成的化合物对肿瘤细胞增殖均有一定的抑制活性,并强于阳性对照药吉非替尼和美洛昔康。

According to combination principle,a series of 1,2-benzothiazine derivatives,which had fragments of Lapatinib and Neratinib were designed and synthesized. Their structures were identified with IR,1H-NMR,13C-NMR and MS. The target compounds were tested for cytotoxic activity against two cancer cell lines,including A549 and MCF-7 by MTT in vitro. All compounds demonstrated certain antitumor abilities,and were better than Gefitinib and Meloxicam.