Yoshimoto M, Miyazawa H, Nakao H, Shinkai K, Arakawa M
J Med Chem. 1979 May;22(5):491-6. doi: 10.1021/jm00191a006.
Antileukemic activities of more than 30 2,5-bis(1-aziridinyl)-p-benzoquinones (4) were correlated against well-defined physicochemical constants. These compounds were evaluated against lymphoid leukemia L1210 in BDF1 mice. The best equations obtained exhibited a linear dependence on the hydrophobic constant, pi. Characteristic aspects of the equations are that the larger the relative hydrophilicity of the drugs the stronger the antileukemic activity will be and that the more hydrophilic compounds have a greater chemotherapeutic index. Steric and electronic effects were also determined to be important. Based on the correlations, three compounds (11, 15 and 19) were designed, synthesized, and biologically evaluated.
30多种2,5-双（1-氮丙啶基）-对苯醌（4）的抗白血病活性与明确的物理化学常数相关。这些化合物在BDF1小鼠中针对淋巴白血病L1210进行了评估。得到的最佳方程显示出与疏水常数π呈线性关系。这些方程的特点是，药物的相对亲水性越大，抗白血病活性越强，且亲水性更强的化合物具有更高的化疗指数。空间和电子效应也被确定为重要因素。基于这些相关性，设计、合成并对三种化合物（11、15和19）进行了生物学评估。
