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A series of 2-methylpyrimido[1,2-a]benzimidazole derivatives has been synthesized in the reactions of 2-aminobenzimidazole (1) with selected halogeno _-diketones: 1,1,1- trifluoro- 2, 1-chloro-1,1-difluoro- 3, 3-chloro-2,4-pentadione- 4 and with 4-fluorobenzoylacetone 5. 2-Aminobenzimidazole (1) in the reactions with _-chloro- and _- bromocinnamaldehyde gave Schiff bases 10 and 11 which have been subjected to reduction using NaBH4 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.
Wydawca
Czasopismo
Rocznik
Tom
Strony
709--716
Opis fizyczny
Bibliogr. 31 poz., rys.
Twórcy
autor
- Department of Technology of Drugs, Wrocław University of Medicine,50-140 Wrocław, Nankier Sq. 1, Poland
autor
- Department of Physical Chemistry, Wroc³aw University of Medicine, 50-140 Wroc³aw, Nankier Sq. 1, Poland
autor
- Department of Technology of Drugs, Wrocław University of Medicine,50-140 Wrocław, Nankier Sq. 1, Poland
autor
- Faculty of Chemistry, University of Wrocław, 50-383 Wrocław, Joliot-Curie Str. 14, Poland
autor
- Department of Experimental Oncology, Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, 53-114 Wrocław, R. Weigla Str. 12, Poland
autor
- Department of Experimental Oncology, Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, 53-114 Wrocław, R. Weigla Str. 12, Poland
autor
- Department of Experimental Oncology, Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, 53-114 Wrocław, R. Weigla Str. 12, Poland
Bibliografia
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- 8.Nawojski A., Prace Naukowe Akademii Medycznej we Wrodawiu, Akademia Medyczna, Wroclaw 5(10) (1969); (in Polish).
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- 23.Gerger C.J., Agy in J.K. and Quada J.C. Jr.; U.S. US 6407131B1 18 Jun 2002; C.A. 137,3330 lz (2002).
- 24.Gerger C.J., Agyin J.K. and Quada J.C. Jr.; U.S. USA6420411 B1 16 Jul 2002; C.A. 137,93753h (2002).
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- 30.Nawrocka W., Liszkiewicz H., Opolski A. and Wietrzyk J., P 362959, 2003.
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Typ dokumentu
Bibliografia
Identyfikator YADDA
bwmeta1.element.baztech-article-BUJ3-0002-0080