Antitumor Agents. 86. Synthesis and Cytotoxicity of α-Methylene-γ-lactone-Bearing Purines

Article abstract of DOI:10.1021/jm00386a025

α-Methylene-γ-lactones covalently linked to adenine (3), hypoxantine (4), and guanine (5) were synthesized by using the convenient Reformatsky-type reaction between ethyl α-(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 most potent (ED50 = 0.3 μg/mL).