Antitumor agents. 86. Synthesis and cytotoxicity of .alpha.-methylene-.gamma.-lactone-bearing purines

Abstract
.alpha.-Methylene-.gamma.-lactones covalently linked to adenine (3), hypoxanthine (4), and guanine (5) were synthesized by using the convenient Reformatsky-type reaction between ethyl .alpha.-(bromomethyl)acrylate and the proper purine ketones. In vitro cytotoxicity data demonstrated that these compounds were active against L-1210 tissue culture cells with 3 being the most potent (ED50 = 0.3 .mu.g/mL).