الفهرس | Only 14 pages are availabe for public view |
Abstract Encouraged by the anticancer activity exhibited by dihydropyrimidines (DHPMs), novel substituted dihydropyrimidine hybrids containing 1,3,4-oxadiazole or coumarin moieties were designed, synthesized and investigated for their cytotoxic activity. The newly synthesized compounds were screened for their in vitro cytotoxic activity against 60 cancer cell lines according to NCI (USA) protocol. The IC50 of compounds 9i, 9k, 9l, 9m, 9n, 9p and 9r have been evaluated against the most sensitive cancer cell lines, leukemia HL-60(TB) and MOLT-4 cell lines. The most active compounds were 9m against HL-60(TB) (IC50= 56 nM) and 9n against MOLT-4 (IC50= 80 nM), more potent than monastrol (IC50= 147 and 215 nM, respectively). Cell cycle analysis of HL-60(TB) cells treated with 9m and MOLT-4 cells treated with 9n showed cell cycle arrest at G2/M phase and pro-apoptotic activity as indicated by annexin V-FITC staining |