2. Academic Validation
  3. Synthesis and antitumor activity of 4-hydroxycoumarin derivatives

Synthesis and antitumor activity of 4-hydroxycoumarin derivatives

  • Bioorg Med Chem Lett. 2004 Nov 15;14(22):5527-31. doi: 10.1016/j.bmcl.2004.09.009.
Jae-Chul Jung 1,  Ji-Ho Lee,  Seikwan Oh,  Jae-Gon Lee,  Oee-Sook Park
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, PO Box 1848, University, MS 38677-1848, USA.
PMID: 15482917 DOI: 10.1016/j.bmcl.2004.09.009
Abstract

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.

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