Synthesis of new xanthone analogues and their biological activity test--cytotoxicity, topoisomerase II inhibition, and DNA cross-linking study.
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.
Woo
Sangwook
S
College of Pharmacy, Catholic University of Daegu, Gyeongsan, Gyeongbuk 712-702, Republic of Korea.
Jung
Ji
J
Lee
Chongsoon
C
Kwon
Youngjoo
Y
Na
Younghwa
Y
D000970:Antineoplastic Agents / Q000138:chemical synthesis; D045744:Cell Line, Tumor; D004249:DNA Damage / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D004852:Epoxy Compounds; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors; D044004:Xanthones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D004852:Epoxy Compounds; D059005:Topoisomerase II Inhibitors; D044004:Xanthones