Dimmock J R, Hamon N W, Noble L M, Wright D E
J Pharm Sci. 1979 Aug;68(8):1033-9. doi: 10.1002/jps.2600680830.
Analogs of some antineoplastic and cytotoxic Mannich bases derived from conjugated styryl ketones were prepared and evaluated for activity in the P-388 lymphocytic leukemia screen. Most of the new compounds had lower antineoplastic and murine toxicity than the parent compounds. Antimicrobial evaluation of some oximes and alcohols related to the Mannich bases revealed activity against certain Gram-positive bacteria and fungi. Primary pharmacological evaluation showed that some compounds containing a dimethylaminomethyl group displayed analgesic and antihistaminic properties. Five of the Mannich bases were evaluated as respiratory inhibitors in mitochondria derived from hepatic tumors, liver tissue from tumor-bearing animals, and normal rat liver. No statistical difference between the sensitivity of the three tissues to the compounds was obtained.
制备了一些由共轭苯乙烯基酮衍生而来的抗肿瘤和细胞毒性曼尼希碱类似物，并在P - 388淋巴细胞白血病筛选中评估其活性。大多数新化合物的抗肿瘤活性和对小鼠的毒性均低于母体化合物。对一些与曼尼希碱相关的肟和醇进行抗菌评估，发现它们对某些革兰氏阳性细菌和真菌具有活性。初步药理学评估表明，一些含有二甲基氨基甲基的化合物具有镇痛和抗组胺特性。对五种曼尼希碱作为源自肝肿瘤、荷瘤动物肝脏组织和正常大鼠肝脏的线粒体中的呼吸抑制剂进行了评估。未获得这三种组织对化合物敏感性之间的统计学差异。
