Synthesis and antitumor activity of 4-hydroxycoumarin derivatives.
A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity. The key fragments were 2a-c, 5c, 12b, 13b, 17, and 18 which were prepared via dianion ring cyclization, Friedel-Crafts acylation, and Reformatsky reaction. Compound 20b showed the most potent antitumor activity among the total 12 derivatives and compounds 19a and 19b exhibited efficacy comparable to etoposide in vitro antitumor activity.
Jung
Jae-Chul
JC
Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, PO Box 1848, University, MS 38677-1848, USA.
Lee
Ji-Ho
JH
Oh
Seikwan
S
Lee
Jae-Gon
JG
Park
Oee-Sook
OS
D015110:4-Hydroxycoumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D015110:4-Hydroxycoumarins; D000970:Antineoplastic Agents