Synthesis of new xanthone analogues and their biological activity test--cytotoxicity, topoisomerase II inhibition, and DNA cross-linking study

  • Bioorg Med Chem Lett. 2007 Mar 1;17(5):1163-6. doi: 10.1016/j.bmcl.2006.12.030.
Sangwook Woo  1 ,  Ji Jung ,  Chongsoon Lee ,  Youngjoo Kwon ,  Younghwa Na
Affiliations
  • 1. College of Pharmacy, Catholic University of Daegu, Gyeongsan, Gyeongbuk 712-702, Republic of Korea.
PMID: 17194586 DOI: 10.1016/j.bmcl.2006.12.030
Abstract

In this report, we prepared some 3-(2',3'-epoxypropoxy)Xanthones and their epoxide ring opened halohydrin analogues, and evaluated their cytotoxicity and Topoisomerase II inhibition activity using doxorubicin and etoposide as references, respectively. Another xanthone compound 9, 1,3-di(2',3'-epoxypropoxy)xanthone, was also synthesized and its DNA cross-linking property including Other two biological activities investigated. The biological test results showed compound 9 possessed excellent cytotoxic and Topoisomerase II inhibitory activity than Other compounds tested. It also exhibited significant DNA cross-linking activities.