| Summary: | A series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and HR-MS. Inhibition of proliferation activities of these derivatives against human leukemia cells (K562), human hepatocellular carcinoma cells (HepG2) and human colon carcinoma cells (HT-29) were evaluated in vitro using the MTT assay. Among the series, compound <b>4l</b> exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC<sub>50</sub> values of 1.75, 3.20, and 4.17 μM, respectively. The morphological, growth inhibitory and apoptosic effects of compound <b>4l</b> in K562 cells, wound healing effect in HepG2 cells, and tube formating effect in matrix gel of HUVEC cells were evaluated consequently. All results indicated that compound <b>4l</b> could be used as a potential antitumor agent in further investigations.
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