2. Academic Validation
  3. Antitumor agents. 86. Synthesis and cytotoxicity of alpha-methylene-gamma-lactone-bearing purines

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

  • J Med Chem. 1987 Mar;30(3):586-8. doi: 10.1021/jm00386a025.
K H Lee,  G K Rice,  I H Hall,  V Amarnath
PMID: 3820231 DOI: 10.1021/jm00386a025
Abstract

alpha-Methylene-gamma-lactones covalently linked to adenine, hypoxanthine, and guanine 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 most potent (ED50 = 0.3 microgram/mL).

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