Synthesis and antitumor activity of 6- and 2-(1-acylsulfanylalkyl)-5,8-dimethoxy-1,4-naphthoquinones

Sixteen novel 6- and 2-（1-acylsulfanylalkyl）-5,8-dimethoxy-l,4-naphthoquinones were designed and synthesized. Their cytotoxicities were evaluated in vitro against BEL-7402, HT-29 and SPC-Al cell lines. The pharmacological results showed that most of the prepared compounds displayed the excellent selectivity for HT-29 cell line. Compound lab exhibited the most potent antitumor activity among the tested compounds.

4-氟苄酰胺类化合物的合成及其对白菜软腐病病菌的抑菌活性研究

以4-氟苄胺和20种酰氯为原料,经过N-酰化反应合成了11个氟苄脂肪酰胺(3A01～3A11)和9个氟苄芳香酰胺类化合物(3B01～3B09),并通过质谱和核磁共振氢谱分析对其结构进行了表征。采用滤纸片法测定了标题化合物对白菜软腐病病菌的抑菌活性,生物测定结果表明,在滤纸片载药量为20μg/disc时,化合物3A01、3A07、3B03和3B09对供试的白菜软腐病病菌有较强的抑菌活性,其抑菌圈直径分别为17、15、15和13 mm。