Dimmock J R, Shyam K, Logan B M, Smith P J, Cross B M
J Pharm Sci. 1984 Apr;73(4):471-7. doi: 10.1002/jps.2600730411.
A number of analogues of 3-dimethylamino-2-dimethylaminomethyl-1-(4-methoxyphenyl)-1-propanone dihydrochloride (IIa) and related compounds which showed activity against P388 lymphocytic leukemia were prepared, and of the 16 analogues, three met the criterion for activity in this screen. The toxicity of IIa was examined in rats and either a single dose of 25 mg/kg or nine daily doses of 12.5 mg/kg administered by the intraperitoneal route produced marked irritation and damage to the tissue with which it came into contact. Compound IIa did not show significant activity against eight other tumor systems.
制备了多种3 - 二甲基氨基 - 2 - 二甲基氨基甲基 - 1 -（4 - 甲氧基苯基）- 1 - 丙酮二盐酸盐（IIa）的类似物以及相关化合物，这些化合物对P388淋巴细胞白血病显示出活性，在这16种类似物中，有三种符合该筛选中的活性标准。在大鼠中检测了IIa的毒性，腹腔注射单剂量25 mg/kg或每日九次剂量12.5 mg/kg均会对与之接触的组织产生明显刺激和损伤。化合物IIa对其他八种肿瘤系统未显示出显著活性。
