Novel 4-(4-substituted phenyl)-5-(3,4,5-trimethoxy/3,4-dimethoxy)-benzoyl-3,4-
dihydropyrimidine-2(1H)-one/thione derivatives (DHP 1–9) were designed, synthesized,
characterized and evaluated for antitumor activity against cancer stem cells. The compounds were
synthesized in one pot. Enaminones E1 and E2 were reacted with substituted benzaldehydes and
urea/thiourea in the presence of glacial acetic acid. The synthesized compounds were characterized
by spectral analysis. The compounds were screened in vitro against colon cancer cell line (LOVO)
Side population (SP) cells mediate chemoresistance in leukemia. However, chemical inhibition
approach to target SP cells has been poorly studied. Herein, we report the discovery of isatin derivatives
of nicotinic acid amide as potent side population cell inhibitors. The selected derivatives showed superior
potency over the reference drug verapamil. Furthermore, the treatment increased chemosensitivity and
inhibited the cell proliferation on three different leukemic cell lines, K562, THP-1 and U937, suggesting