2. Academic Validation
  3. Synthesis and biological evaluation of new 4β-anilino-4'-O-demethyl-4-desoxypodophyllotoxin derivatives as potential antitumor agents

Synthesis and biological evaluation of new 4β-anilino-4'-O-demethyl-4-desoxypodophyllotoxin derivatives as potential antitumor agents

  • Eur J Med Chem. 2011 Jan;46(1):285-96. doi: 10.1016/j.ejmech.2010.11.016.
Li Wang 1,  Fenyan Yang,  Xiaochun Yang,  Xianghong Guan,  Chunqi Hu,  Tao Liu,  Qiaojun He,  Bo Yang,  Yongzhou Hu
Affiliations

Affiliation

  • 1 ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
PMID: 21145139 DOI: 10.1016/j.ejmech.2010.11.016
Abstract

A series of new 4β-anilino-4'-O-demethyl-4-desoxypodophyllotoxin derivatives were prepared and evaluated for their cytotoxicities against four human Cancer cell lines including KB, KB/VCR, A549 and 95D. Most compounds showed better growth-inhibition activities against tested cell lines than that of etoposide (VP-16). Preliminary structure-activity relationships (SARs) were concluded and it indicated that the side chains substituted at 4β position of podophyllotoxin significantly influenced the cytotoxic activity, especially for the drug resistance profile. In vivo studies of compound 26c on highly metastatic human lung Cancer xenograft in nude mice showed that it can significantly inhibit tumor growth with administrating by oral route.

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