2. Academic Validation
  3. Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones

Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones

  • Bioorg Med Chem. 2007 Feb 15;15(4):1651-8. doi: 10.1016/j.bmc.2006.12.012.
Hee-Kyung Rhee 1,  Hyen Joo Park,  Sang Kook Lee,  Chong-Ock Lee,  Hea-Young Park Choo
Affiliations

Affiliation

  • 1 School of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
PMID: 17194596 DOI: 10.1016/j.bmc.2006.12.012
Abstract

Benzofuroquinolinediones (7c and 7d) were synthesized by base-catalyzed condensation of dichloroquinolinediones with phenolic derivatives. Their dialkylaminoalkoxy derivatives (8i-8p) were prepared by reaction with various dialkylaminoalkyl chlorides. The cytotoxicity of the synthesized compounds was evaluated against eight types of human Cancer cell lines, and their Topoisomerase II inhibition was assessed. In general, the cytotoxicity of benzofuroquinolinediones (8i-8p) was similar or superior to that of doxorubicin and showed more potent inhibitory activity than naphthofurandiones (8a-8h). Also, most of the compounds exhibited excellent Topoisomerase II inhibitory activity at a concentration of 5 microM and two compounds, 8d and 8i, showed IC50 values of 1.19 and 0.68 microM, respectively, and were much more potent than etoposide (IC50=78.4 microM), but similar to doxorubicin (IC50=2.67 microM). However their inhibitory activity on Topoisomerase I was lower, and 8d and 8i showed IC50 values of 42.0 and 64.3 microM, respectively.

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