Abstract: In order to find novel anthraquinone compounds with high fungicidal activity, a series of novel physcion-amino acid derivatives 2a-6p were designed and synthesized by introducing the amino acids into the lead compound physcion by etherification, hydrolysis and acid chloride reaction according to the method of active substructure combination. The structures of the target compounds were confirmed by ¹H NMR and HRMS. The preliminary bioassay data showed that all the target products exhibited certain fungicidal activities against the six kinds of plant pathogens at 0.2 mmoL/L. Compounds 6e had the highest inhibitory activities against Rhizoctonia solani and Colletotrichum gloeosporioides with 69.93% and 67.18%, respectively. Compounds 5a, 6a and 6c had moderate inhibitory activities against R. solani with 60.51%, 53.28% and 58.50%, respectively. The inhibitory activities of compounds 6a and 6c against C. gloeosporioides were 49.25% and 47.61%, respectively. The above compounds showed significantly higher fungicidal activities than the lead compound physcion. The preliminary analysis of structure effective relationship showed that the introduction of amino acids at the hydroxyl position of physcion could enhance its fungicidal activity against R. solani, Pyricularia oryzae, Sclerotinia sclerotiorum, Botrytis cinerea Alteraria alternate and C. gloeosporioide.