Bollag W
Chemotherapy. 1975;21(3-4):236-47. doi: 10.1159/000221864.
The properties of a new aromatic retinoic acid analog are described. The compound: all-trans-N-ethyl-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenamide = Ro 11-1430, exerts a therapeutic influence on chemically induced papillomas and carcinomas of the skin of mice. It leads to a marked regression of chemically induced epithelial tumors but does not inhibit the growth of transplantable tumors. The therapeutic use of retinoic acid and its analogs is limited by the appearance of the toxic side effects of the so-called hypervitaminosis A syndrome. The relationship between the anti-tumor activity and these toxic effects is considered a good inidicator for establishing the quality of a compound. The new retinoic acid analog posses a ten times more favorable therapeutic ratio than retinoic acid. The mechanism of action is discussed.
描述了一种新型芳香维甲酸类似物的性质。该化合物:全反式-N-乙基-9-(4-甲氧基-2,3,6-三甲基苯基)-3,7-二甲基-2,4,6,8-壬四烯酰胺 = Ro 11-1430,对化学诱导的小鼠皮肤乳头瘤和癌具有治疗作用。它可导致化学诱导的上皮肿瘤明显消退,但不抑制可移植肿瘤的生长。维甲酸及其类似物的治疗应用受到所谓维生素A过多综合征毒性副作用出现的限制。抗肿瘤活性与这些毒性作用之间的关系被认为是确定化合物质量的良好指标。新型维甲酸类似物的治疗指数比维甲酸高十倍。并讨论了其作用机制。