[Studies of chemopreventive agents against neoplasma: synthesis of 3-acetyl coumarin derivatives and relationship between antimutagenic activity and structure].
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.
Huang
X L
XL
Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing.
Xu
S P
SP
Fu
Z D
ZD
An
B
B
D016587:Antimutagenic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009152:Mutagenicity Tests; D013329:Structure-Activity Relationship
D016587:Antimutagenic Agents; D000970:Antineoplastic Agents; D003374:Coumarins; C094809:3-acetylcoumarin