本文選題：-硒唑 + 多雜環(huán)��； 參考：《有機(jī)化學(xué)》2017年02期

【摘要】：以取代1,3-硒唑?yàn)槟０?分別利用1,2,4-三唑、四唑、VA二唑、吡唑、1,2,4-三嗪和丁二酰亞胺等修飾,首次設(shè)計合成了6類共22個目標(biāo)分子,并利用IR,NMR和HRMS等波譜技術(shù)對目標(biāo)分子進(jìn)行了結(jié)構(gòu)表征.評價了目標(biāo)分子對Cdc25B的抑制活性,結(jié)果發(fā)現(xiàn),13個目標(biāo)分子具有較好的抑制活性,其中有5種目標(biāo)分子的抑制活性高于陽性參照物Na_3VO_4有望成為抗腫瘤藥物先導(dǎo)物.構(gòu)效分析結(jié)果發(fā)現(xiàn),在1,3-硒唑骨架上引入多氮雜環(huán)三唑、四唑和三嗪,引入含有氨基和巰基的噻二唑和VA二唑等有望獲得活性優(yōu)良的新型含硒有機(jī)分子.
[Abstract]:Six kinds of 22 target molecules were designed and synthesized by using substituted 1 ~ (3) -selenazole as template, using 1 ~ (2) C _ (2) -triazole, tetrazolium VA diazole, pyrazole 1 ~ (2 +) ~ (22) -triazine and succinimide, respectively, for the first time, a total of 22 target molecules of 6 classes were designed and synthesized. The structure of the target molecule was characterized by IR NMR and HRMS. The inhibitory activity of the target molecule against Cdc25B was evaluated. The results showed that 13 target molecules had better inhibitory activity, and 5 of them had higher inhibitory activity than the positive reference Na3VOS4, which was expected to be the leader of antitumor drugs. The results of structure-activity analysis showed that polyazacyclic triazole, tetrazole and triazine, thiadiazoles containing amino groups and thiadiazole and VA diazole could be added to the skeleton of 1-azo-3-selenazole to obtain novel selenium-containing organic molecules with good activity.
【作者單位】： 遼寧師范大學(xué)化學(xué)化工學(xué)院;
【基金】：遼寧省教育廳科學(xué)技術(shù)研究(No.2009A426)資助項(xiàng)目~~
【分類號】：O627.61;TQ460.1

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