Dubois R J, Lin C C, Michel B L
J Pharm Sci. 1975 May;64(5):825-9. doi: 10.1002/jps.2600640521.
No information is available on the structural requirements for the antitumor activity of sparsomycin, an antibiotic obtained from the fermentation broth of Streptomyces sparsogenes. Its high in vivo and in vitro activity, novel structure, and uncommon mode of action have, therefore, suggested the synthesis of analogs. This report describes the preparation and screening of a series of N-substituted 3-aryl acrylamides which are closely related to sparsomycin. Three compounds exhibited some tumor inhibition but insufficient to warrant further testing.
关于从浅黄链霉菌发酵液中获得的抗生素 sparsomycin 的抗肿瘤活性的结构要求尚无信息。因此，其高体内和体外活性、新颖的结构以及不寻常的作用方式提示了类似物的合成。本报告描述了一系列与 sparsomycin 密切相关的 N-取代 3-芳基丙烯酰胺的制备和筛选。三种化合物表现出一定的肿瘤抑制作用，但不足以保证进一步测试。
