Sparsomycin Analogs. IV. : Synthesis and Antitumor Activity of Pyrimidine-5-carboxamides and (E)-β-(Pyrimidin-5-yl)-acrylamides

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Various pyrimidine-5-carboxamides (14,16,18,20,and 21) and (E)-β-(pyrimidin-5-yl)acrylamides (15,17,19,and 22)were synthesized as sparsomycin analogs, and their antitumor activity was examined by cell growth inhibition assay against mouse leukemia L5178Y cells in vitro.Synthesis was carried out by condensation of appropriate acids (4,6,10,and 12) and amino acid methyl esters (13) by the mixed anhydride method using isobutyl chlorocarbonate. The condensation product was converted to the corresponding acid and alcohol derivatives by hydrolysis and LiBH_4 reduction. The compounds having an ethylene linkage at the C-5 position and an ester moiety at the terminal amino acid functionality (15b, and 17b-g) exhibited remarkable antitumor activity.
社団法人日本薬学会の論文
1988-06-25