Development of a fat soluble signal molecule for cancer chemotherapy

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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.