Atwell G J, Rewcastle G W, Baguley B C, Denny W A
Cancer Research Laboratory, University of Auckland School of Medicine, New Zealand.
Anticancer Drug Des. 1989 Aug;4(2):161-9.
A number of structural analogues of the solid tumour active drug flavoneacetic acid have been prepared and evaluated for in vivo activity against colon 38 adenocarcinoma, in order to extend the limited structure-activity relationships available for compounds with this type of activity. Apart from the fused ring analogue xanthenone-4-acetic acid, structural and electronic modifications of the nucleus led to inactive compounds, suggesting the existence of quite narrow structure-activity relationships.
为了扩展针对具有此类活性的化合物有限的构效关系,已制备了多种实体瘤活性药物黄酮乙酸的结构类似物,并对其抗结肠38腺癌的体内活性进行了评估。除了稠环类似物呫吨酮-4-乙酸外,核的结构和电子修饰导致化合物无活性,这表明存在相当狭窄的构效关系。