Varnavas A, Nisi C, Lassiani L, Sava G, Perissin L, Boccù E
Department of Pharmaceutical Sciences, University of Trieste, Italy.
Arzneimittelforschung. 1991 Nov;41(11):1168-72.
The hydrosoluble triazene derivatives of phenylacetic, phenylbutyric and cinnamic acid have been synthesized and their logP and pKa values were simultaneously determined according to a multiparametric fitting of potentiometric data. The antitumor activity caused by the synthesized compounds in mice bearing either Lewis lung carcinoma or TLX5 lymphoma was evaluated and discussed in comparison with the parent compound (p-(3,3-dimethyl-1-triazeno)benzoic acid potassium salt (DM-COOK, CAS 70055-49-1). The tested compounds were at least as active as DM-COOK, the cinnamic and the phenylacetic derivatives being the more active compounds in mice bearing TLX5 lymphoma and Lewis lung carcinoma, respectively.
已合成了苯乙酸、苯丁酸和肉桂酸的水溶性三氮烯衍生物，并根据电位数据的多参数拟合同时测定了它们的logP和pKa值。与母体化合物（对-(3,3-二甲基-1-三氮烯)苯甲酸钾盐(DM-COOK, CAS 70055-49-1)）相比，评估并讨论了合成化合物对携带Lewis肺癌或TLX5淋巴瘤的小鼠的抗肿瘤活性。所测试的化合物至少与DM-COOK活性相当，肉桂酸和苯乙酸衍生物分别是对携带TLX5淋巴瘤和Lewis肺癌的小鼠中活性更高的化合物。
