以取代硫色满酮(1a-1f)和盐酸苯肼(2)为原料,经Borsche-Drechsel环化反应合成了6个6,11-二氢苯并噻喃并[4,3-b]吲哚类化合物(3a-3f);3a-3f用间氯过氧苯甲酸氧化成5,5-二氧-6,11-二氢苯并噻喃并[4,3-b]吲哚类化合物(4a-4f),其结构经1H NMR,IR和HR-ESI-MS确证。采用MTT法初步测定了1,3和4对肺癌细胞A549的抑制作用。结果表明:3a-4f的抑制活性均强于1。
6,11-Dihydrobenzothiopyrano[4,3-b]indole compounds[4,3-b]indoles(3a - 3f) were synthesized by Borsche-Drechsel cyclization reaction of substituted thiochromanones(1a - 1f) and phenylhydrazine hydrochloride(2).Their oxidative products(4a - 4f) were obtained by oxidation reaction of 3a - 3f using m-chloroperoxybenzoic acid as the oxidizer.The structures were confirmed by1 H NMR,IR and HR-ESI-MS.The anti-tumor activities of 1,3 and 4 against A549 were investigated by MTT method.The results showed that 3a - 4f exhibited better anti-tumor activities than 1.