Dimmock J R, Taylor W G
J Pharm Sci. 1975 Feb;64(2):41-9. doi: 10.1002/jps.2600640210.
A number of nuclear-substituted styryl ketones, the related Mannich bases, and allyl alcohols were synthesized and evaluated for antitumor activity, principally in the L-1210 lymphoid leukemia and P-388 lymphocytic leukemia screening tests. The cytotoxicity of some of these compounds assessed in Eagle's 9KB carcinoma cell culture system was also recorded. Two of the Mannich bases showed promising levels of activity in the P-388 screening; of the results obtained to date, over one-third of the derivatives showed cytotoxicity at dose levels of 1-3 ppm. Other pharmacological results of these compounds are briefly reported.
合成了多种核取代苯乙烯基酮、相关的曼尼希碱和烯丙醇,并对其进行了抗肿瘤活性评估,主要是在L - 1210淋巴细胞白血病和P - 388淋巴细胞白血病筛选试验中。还记录了其中一些化合物在伊格尔9KB癌细胞培养系统中评估的细胞毒性。其中两种曼尼希碱在P - 388筛选中显示出有前景的活性水平;在迄今为止获得的结果中,超过三分之一的衍生物在1 - 3 ppm的剂量水平下显示出细胞毒性。简要报道了这些化合物的其他药理结果。