The present invention provides chemical entities or compounds and pharmaceutical compositions thereof are selective anticancer agents over a panel of human cancer cell lines and useful for the treatment of cancer. This invention is in the field of medicinal chemistry and relates to methods of preparing thiourea/benzothiazole coumarin compounds as formula I, II, wherein R is methyl and phenyl wherein Ri is mono or disubstituted electron donating and withdrawing groups. wherein formula I: R is selected from the group consisting of: CH3,C6H5 Ri is selected from the group consisting of: H, 4-C1, 4-Br, 4-CH3, 2-C1, 2,4-diCl, 2-CH3, 2-N02, 2- F, 2-Br. wherein formula II: R is selected from the group consisting of: CH3,C6H5 Ri is selected from the group consisting of: H, 6- C1, 6-Br, 6-CH3,4-C1, 4,6-diCl, 4-CH3, 4-N02, 4-F, 4-Br 1