Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 25, Issue 15, Pages 4133-4144Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.06.001
Keywords
DNA topoisomerase; Nucleoside; Antiproliferative activity; Cancer
Funding
- Ministry of Education, Culture, Sports, Science and Technology, Japan
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We developed novel nucleoside-based topoisomerase II selective inhibitors and showed that small structural units, such as catechols, are essential for DNA topoisomerase II inhibitory activity. Moreover, nucleoside analogues containing TBS and 1,3-dithian moieties had potent and selective DNA topoisomerase II inhibitory activities. In further experiments, compound 25b having a beta configuration of the thymine moiety showed relatively strong growth inhibitory activity against cancer cell lines, and was more potent against all cancer cell lines than compound 26b, which carries a thymine moiety in the alpha configuration. (C) 2017 Elsevier Ltd. All rights reserved.
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