2. Academic Validation
  3. Discovery of Novel Topoisomerase II Inhibitors by Medicinal Chemistry Approaches

Discovery of Novel Topoisomerase II Inhibitors by Medicinal Chemistry Approaches

  • J Med Chem. 2018 Oct 25;61(20):8947-8980. doi: 10.1021/acs.jmedchem.7b01202.
Wei Hu 1,  Xu-Sheng Huang 2,  Ji-Feng Wu 3,  Liang Yang 4,  Yong-Tang Zheng 2,  Yue-Mao Shen 4,  Zhi-Yu Li 5,  Xun Li 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Microbial Technology, School of Life Science , Shandong University , 27 South Shanda Road , 250100 Ji'nan , Shandong , P. R. China.
  • 2 Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science and Yunnan Province , Kunming Institute of Zoology, Chinese Academy of Sciences , Kunming , Yunnan 650223 , China.
  • 3 Institute of Criminal Science and Technology , Ji'nan Public Security Bureau , 21 South QiliShan Road , 250000 Ji'nan , Shandong , P. R. China.
  • 4 Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , 44 West Culture Road , 250012 , Ji'nan , Shandong , P. R. China.
  • 5 Department of Pharmaceutical Sciences , Philadelphia College of Pharmacy , Philadelphia , Pennsylvania 19104 , United States.
PMID: 29870668 DOI: 10.1021/acs.jmedchem.7b01202
Abstract

DNA Topoisomerase II (Topo II) is an important Enzyme involved in DNA replication, recombination, and repair. Despite the popular applications of Topo II inhibitors in Cancer therapy, there is still an urgent need to upgrade Topo II inhibitors to cope with drug resistance and severe adverse effects. Accordingly, novel Topo II catalytic or multitarget Topo II inhibitors are gaining more attention and make it possible to ease the toxic limitations of Topo II poisons. In this review, medicinal chemistry approaches are mainly discussed toward the development of potent Topo II inhibitors with low toxicities.

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