Sparsomycin analogs. V. Synthesis and antitumor activity of (E)-. BETA.-(pyrimidin-5-yl) acrylamides.

…, A WADA, Y HAMAOKA, S NAGAI, S FUKUDA…

Index: Kanatomo; Wada; Hamaoka; Nagai; Fukuda; Tanaka; Sasaki Chemical and Pharmaceutical Bulletin, 1988 , vol. 36, # 11 p. 4421 - 4425

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Abstract

Various (E)-β-(pyrimidin-5-yl) acrylamides (4 and 5) were synthesized as sparsomycin analogs, and the relationship between chemical structure and antitumor activity was examined. Synthesis involved condensation of appropriate acids (3) and methyl methioninate (L and D isomers) by the mixed anhydride method using isobutyl chlorocarbonate. The antitumor activity was studied by [methyl-3 H] thymidine ...