{Author}: Junjie Ma；Gang Hu；Lijun Xie；Lei Chen；Boxuan Xu；Ping Gong*

{Journal}: Chemical Research in Chinese Universities

{Year}: 2015

{Volume}: 31

{Issue}: 6

{Pages}:958-963

{Keywords}: Benzothiazole；Semicarbazone；Antitumor activity

{Abstract}: A series of novel benzothiazole derivatives bearing semicarbazone as a linker was designed and synthesized, and their in vitro antitumor activities were evaluated against four cancer cell lines(HT29, H460, A549 and MDA-MB-231). Most of them showed moderate to excellent activity against all the tested cell lines. Among them, compounds 12 a― 12 i with fluoro-substituted benzyl-1 H -indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12 d exhibited excellent antitumor activity with IC₅₀ values of 0.015, 0.28, 1.53 and 0.68 μmol/L against the four tested cell lines respectively.