Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Synthesis and in Vitro Antiproliferative Evaluation of Novel Hybrids from 1,3,4-Thiadiazole and Benzisoselenazolone
Fen JingXiaoyun FuSha LiBaolin LiJijun ZhaoXuefeng WangYuming LiuBaoquan Chen
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2015 Volume 63 Issue 6 Pages 431-437


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 µM. Compounds 4b and 4m displayed highly effective biological activities against MCF-7 cells with an IC50 values of 2.03 and 2.06 µM, respectively. Compound 4i exhibited the best inhibitory effect against A549 cells with an IC50 value of 1.03 µM.

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© 2015 The Pharmaceutical Society of Japan
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