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KMID : 0043319960190030235
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Archives of Pharmacal Research
1996 Volume.19 No. 3 p.235 ~ p.239
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Synthesis and antitumor evaluation of α-Methylene-r-bu-tyrolactone-Linked to 5-substituted uracil nucleic acid bases
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Kim Jack-C.
Kim Ji-A
Kim Si-Hwan
Park Jin-Il
Kim Seon-Hee
Park Soon-Kyu
Park Won-Woo
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Abstract
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Six, heretofore undescribed, were synthesized and evaluated against three cell lines (FM-3A, P-388 and U-937). For the preparation of .alpha.-methylene-.gamma.-butyrolactone bearing 5-substituted uracils (6a-f), the effcient Reformatsky type reaction was employed which involves the treatment of ethyl .alpha.(bromomethyl) acrylate and zinc with the respective 5-substituted uracil-1-ylacetones (5a-f). The acetone derivatives (5a-f) were directly obtained by the respective alkylation reaction of 5-substituted uracils with chloroacetone in the presence of (or NaH). These lactone compounds 6a-f exhibited moderate to significant activity in all of the three cell lines, and 6b, 6c and 6e showed significant antitumor activities (inhibitory concentrations () ranged from 1.3-3.8 .mu.g/ml.
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