Structure and antitumor activity relationship of 2-arylidene-4-cyclopentene-1, 3-diones and 2-arylideneindan-1, 3-diones.
A series of 2-arylidene-4-cyclopentene-1,3-diones and 2-arylideneindan-1,3-diones, as well as mono- and bis(arylidene substituted)cycloalkanones, was synthesized and examined for antitumor activity against ascites sarcoma-180. All the 2-arylidene-4-cyclopentene-1,3-diones and one arylideneindan-1,3-dione (where the arylidene group was either a hydroxybenzylidene or substituted hydroxybenzylidene) exhibited a high degree of activity. Among both types of 1,3-diones and 3-methoxy-4-hydroxybenzylidene derivatives were found to possess the greatest potency, while all the mono- and bis(arylidene)cycloalkanones were found to be inactive.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000627:therapeutic use; D005260:Female; D007192:Indenes / Q000138:chemical synthesis*; D007659:Ketones / Q000138:chemical synthesis / Q000627:therapeutic use; D051379:Mice; D012510:Sarcoma 180 / Q000188:drug therapy; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D003517:Cyclopentanes; D007192:Indenes; D007659:Ketones