沙利度胺衍生物的设计合成及其抗肿瘤活性研究

目的设计合成1，3-二氢-1，3-二氧代．2H-异吲哚-N-取代沙利度胺衍生物。并对其进行体外抗肿瘤活性测试。方法以2．氨基-β-D-吡喃葡萄糖盐酸盐为原料，经过6步反应得到化合物N-（3’，4’，6＇-三乙酰-1’-溴代吡喃葡萄糖）-1,3-二氢-1，3-二氧代-2H-异吲哚，该化合物经过溴代、取代反应得到目标化合物。通过对4T1细胞存活率的测试测定20个目标化合物体外抗肿瘤活性。结果设计合成的20个目标化合物均未见文献报道。所有化合物均经过1H-NMR谱确证，部分化合物经IR、MS谱确证。结论所有目标化合物对4T1细胞均具有-定的抑制生长作用。表明所合成的沙利度胺衍生物均有-定的抗肿瘤活性。

Design, synthesis, and antitumor activity of thalidomide derivatives

Aim To study antitumor activity of thalidomide derivatives. Method According to the structure of thalidomide, start from -D -Glucosamine Hydrochloride, twenty compounds were designed and synthesized. All of them were confirmed by 1H-NMR and parts of them were confirmed by IR, MS spectra; all of them were tested by measuring the percent of survival of 4T1 cell. Results All the compounds were first reported, and the preliminary anticancer test showed that all the designed compounds have extent antitumor activity. Conclusion The derivatives substituted by 3,4,6-tri-O-acetyl glucopyrannoside have better anticancer activity than thalidomide dose.