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  2. Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020)

Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020)

  • Eur J Med Chem. 2020 Dec 15:208:112830. doi: 10.1016/j.ejmech.2020.112830.
Jiaqi Xiao 1 Meixiang Gao 1 Zhou Sun 1 Qiang Diao 2 Peng Wang 3 Feng Gao 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Biobased Material and Green Papermaking (LBMP), Qilu University of Technology (Shandong Academy of Sciences), Jinan, PR China.
  • 2 Department of Medical Imaging, Jinling Hospital, Medical School of Nanjing University, Nanjing, PR China.
  • 3 Department of Radiology, The First Affiliated Hospital of USTC, Division of Life Sciences of Medicine, University of Science and Technology of China, Hefei, PR China. Electronic address: peng615wang@163.com.
  • 4 State Key Laboratory of Biobased Material and Green Papermaking (LBMP), Qilu University of Technology (Shandong Academy of Sciences), Jinan, PR China; Department of Medical Imaging, Jinling Hospital, Medical School of Nanjing University, Nanjing, PR China. Electronic address: rggaofeng@hotmail.com.
Abstract

Podophyllotoxins and epipodophyllotoxins, possess excellent activity against both drug-sensitive and drug-resistant even multidrug-resistant Cancer cells via inhibition of tubulin polymerization. Several podophyllotoxin/epipodophyllotoxin derivatives such as etoposide and teniposide have already been applied for Cancer therapy, revealing their potential as putative Anticancer drugs. Hybridization of podophyllotoxin/epipodophyllotoxin moiety with other Anticancer pharmacophores is a promising strategy to develop novel drug candidates so as to overcome drug resistance and improve the specificity, and numerous of podophyllotoxin/epipodophyllotoxin hybrids exhibit excellent in vitro antiproliferative and in vivo Anticancer potency. This review emphasizes the recent development of podophyllotoxin/epipodophyllotoxin hybrids with potential application for Cancer therapy covering articles published between 2010 and 2020. The mechanisms of action, the critical aspects of design as well as structure-activity relationships were also summarized.

Keywords

Anticancer; Drug resistance; Epipodophyllotoxin; Hybrid compounds; Mechanism of action; Podophyllotoxin; Structure-activity relationship.

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