Edwards M L, Stemerick D M, Sunkara P S
Merrell Dow Research Institute, Cincinnati, Ohio 45215.
J Med Chem. 1990 Jul;33(7):1948-54. doi: 10.1021/jm00169a021.
A series of chalcones was evaluated as antimitotic agents. One of these, (E)-1-(2,5-dimethoxyphenyl)-3-[4-(dimethylamino)phenyl]-2-methyl-2-pr open- 1-one) (73), was found to be an effective antimitotic agent at a concentration of 4 nM in an in vitro HeLa cell test system. When evaluated in experimental tumor models in vivo, this compound exhibited antitumor activity against L1210 leukemia and B16 melanoma.
一系列查耳酮被评估为抗有丝分裂剂。其中之一,(E)-1-(2,5-二甲氧基苯基)-3-[4-(二甲基氨基)苯基]-2-甲基-2-丙烯-1-酮(73),在体外HeLa细胞测试系统中,浓度为4 nM时被发现是一种有效的抗有丝分裂剂。在体内实验性肿瘤模型中进行评估时,该化合物对L1210白血病和B16黑色素瘤表现出抗肿瘤活性。