Synthesis and in Vitro Antiproliferative Evaluation of Novel Hybrids from 1,3,4-Thiadiazole and Benzisoselenazolone

CHEMICAL & PHARMACEUTICAL BULLETIN(2015)

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摘要
Novel hybrids from 1,3,4-thiadiazole and benzisoselenazolone were designed, synthesized and evaluated for their in vitro antiproliferative activities by CCK-8 assay against three types of human cancer cell lines, SMMC-7721, MCF-7 and A549 cells. The preliminary bioassay results demonstrated that all tested compounds 4a-p showed potent antiproliferative activities, and some compounds exhibited better effects than positive control ethaselen and 5-fluorouracil (5-FU) against various cancer cell lines. Furthermore, compound 4g showed significant antiproliferative activities against SMMC-7721 cells with an IC50 value of 2.08 mu M. Compounds 4b and 4m displayed highly effective biological activities against MCF-7 cells with an IC50 values of 2.03 and 2.06 mu M, respectively. Compound 4i exhibited the best inhibitory effect against A549 cells with an IC50 value of 1.03 mu M.
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关键词
synthesis,1,3,4-thiadiazole,benzisoselenazolone,ebselen,ethaselen,antiproliferative activity
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