Development of a fat soluble signal molecule for cancer chemotherapy

香叶基香叶酸(GGA)是一种维甲酸类似物，因此人们合成了多种GGA类似物，并对其生物活性进行了评价。共轭多烯体系和甲基取代基的位置结合在一起对HL-60细胞的基因转录和诱导凋亡活性具有重要的调控作用。这些高活性可能是由于与受体的高结合亲和力造成的。这些结果为GGA衍生物作为非环维A酸类似物的构效关系提供了有用的信息，为新药的开发提供了有用的信息。

As geranylgeranoic acid (GGA) was considered as an retinoic acid analog, various GGA analogs were efficiently synthesized and their biological activities were evaluated. The combination of conjugate polyene system and the position of methyl substituent played an important role in regulation of gene transcription and apoptosis-inducing activity in HL-60 cells. These high activities would be caused by high binding affinity to the receptors. The results provide useful information on the structure-activity relationship of GGA derivatives as mimic of acyclic retinoic acid analogs for the development of new drugs.