A novel and efficient synthetic route to α-aminophosphonates containing benzothiazole moiety via a cascade three-component reaction from conveniently available starting materials has been developed. The target compounds 3a-3g, 7 and 8a, 8b were evaluated for their anticancer activities against the cancer cell line HL-60 in vitro by the MTT method. Compound 3g showed good cancer inhibitory activity against the tested cell line. Further study is necessary to find out the potential antitumor activities.
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