抗肿瘤剂。86. 含α-亚甲基-γ-内酯嘌呤的合成及细胞毒性
Antitumor agents. 86. Synthesis and cytotoxicity of alpha-methylene-gamma-lactone-bearing purines.
作者信息
Lee K H, Rice G K, Hall I H, Amarnath V
出版信息
J Med Chem. 1987 Mar;30(3):586-8. doi: 10.1021/jm00386a025.
PMID:3820231
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).
摘要
通过α-(溴甲基)丙烯酸乙酯与适当的嘌呤酮之间便捷的类Reformatsky反应，合成了与腺嘌呤、次黄嘌呤和鸟嘌呤共价连接的α-亚甲基-γ-内酯。体外细胞毒性数据表明，这些化合物对L-1210组织培养细胞具有活性，其中化合物3活性最强（半数有效剂量ED50 = 0.3微克/毫升）。
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