Synthesis and Antiproliferative Activity in vitro of New 2-Aminobenzimidazole Derivatives.Part 2 [1]

摘要

A series of 2-methylpyrimido[1,2-a]benzimidazole derivatives has been synthesized in the reactions of 2-aminobenzimidazole(1)with selected halogeno beta-diketones:1,1,1-trifluoro-2,1-chloro-1,1-difluoro-3,3-chIoro-2,4-pentadione-4 and with 4-fluoro-benzoylacetone 5.2-Aminobenzimidazole(1)in the reactions with alpha-chloro-and "-bromocinnamaldehyde gave Schiff bases 10 and 11 which have been subjected to reduction using NaBH_4 and 3-benzylideno-1,2-dihydro-(12)and 3-benzylideno-1,2,9,10-tetrahydroimidazo[1,2-a]benzimidazole(13)were obtained.The structures 2-13 were identified by the results of elemental analysis and their IR,~1H NMR and MS spectra.Compounds 2-13 were examined for their antiproliferative activity in vitro against the cells of 3 human cancer cell lines,using SRB(sulphorhodamine B)or MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide)technique.Four out of all tested compounds revealed cytotoxic activity in vitro.