Studies of chemopreventive agents against neoplasma: synthesis of 3-acetyl coumarin derivatives and relationship between antimutagenic activity and structure
Huang, X.L.; Xu, S.P.; Fu, Z.D.; An, B.
Yao Xue Xue Bao 31(6): 431-436
1996
ISSN/ISBN: 0513-4870 PMID: 9275723 Document Number: 456892
Twenty-five 3-acetylcoumarin derivatives were synthesized among which twenty-two were not reported before. Antimutagenic activity screen in vitro has shown that some of these compounds have various activities. The structure and activity relationship for 5-, 7-, 8-substituents has been studied. Pharmacological data showed that: the substituent on position 8 has important effect on its activity. When there is only a hydroxy group on position 7, its activity is the highest among those with other substituents, but when a methyl is on position 8, the order of the activity is reversed. Other trends have also been found which provided some clues for further structural modification.