Chemical and Pharmaceutical Bulletin p. 964 - 973 (2000)
Update date:2022-07-29
Topics:
Chang, Chiung-Yun
Huang, Li-Jiau
Wang, Jih-Pyang
Teng, Che-Ming
Chen, Sheng-Chih
Kuo, Sheng-Chu
In a continuation of our search for novel anti-platelet agents, isoflavone quinone and isoflavanquinone were selected as lead compounds and the synthesis of their methoxy derivatives was carried out. Among them, the 4'- and 7-methoxy derivatives were successfully prepared, whereas the attempt to obtain 3'-methoxy derivatives resulted in their isomers, 3'-methoxyflavone quinone and 3'-methoxyflavanquinone, instead. After screening for their anti-platelet, anti-inflammatory and anti-allergic activities, a preliminary structure-activity relationship was established. Compounds 6c, 7a - c, 8c and 9a - c were found to exhibit significant activities. In particular, compound 7c demonstrated very potent anti-platelet, anti-inflammatory and anti-allergic activities and was then recommended for further pharmacological investigation.
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