2. Academic Validation
  3. Synthesis and Biological evaluation of novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxins as anticancer compounds

Synthesis and Biological evaluation of novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxins as anticancer compounds

  • Bioorg Med Chem Lett. 2015 Jul 15;25(14):2860-3. doi: 10.1016/j.bmcl.2015.04.053.
Irfan Hyder 1,  Deepthi Yedlapudi 2,  Shasi V Kalivendi 3,  Jabeena Khazir 4,  Tabasum Ismail 4,  Naresh Nalla 5,  Sreekanth Miryala 1,  Halmuthur M Sampath Kumar 6
Affiliations

Affiliations

  • 1 NPC Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India; Academy of Scientific and Innovative Research, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • 2 Centre for Chemical Biology Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • 3 Centre for Chemical Biology Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: kalivendi@iict.res.in.
  • 4 Medicinal Chemistry Division, Indian Institute of Integrative Medicine, Jammu 180001, India.
  • 5 NPC Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India.
  • 6 NPC Division, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India; Academy of Scientific and Innovative Research, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: sampath@iict.res.in.
PMID: 26022842 DOI: 10.1016/j.bmcl.2015.04.053
Abstract

A series of novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxin derivatives were synthesized by employing azide-nitrile Click Chemistry approach. All the derivatives were evaluated for their cytotoxicity against a panel of four human Cancer cell lines and their IC50 values were found to be in the range of 2.4-29.06 μM. The cytotoxicity exhibited by the majority of test compounds were found to comparable and often more effective than doxorubicin and all compounds exhibited higher cytotoxicity on A-549 cell lines. Cell cycle analysis showed that the novel 4β-[(5-substituted)-1,2,3,4-tetrazolyl] podophyllotoxins resulted in cell cycle arrest at G2/M phase and were also found to be the potent inhibitors of tubulin polymerization in vitro.

Keywords

Anticancer activity; Tetrazolyl podophyllotoxin; Tubulin polymerization.

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