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Sixteen novel 6-and 2-(1-aeylsulfanylalkyl)-5,8-dimethoxy-1,4-naphthoquinones were designed and synthesized.Their eytotoxicifies 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 16b exhibited the most potent antitumor activity among the tested compounds.