2. Academic Validation
  3. Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents

Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents

  • Bioorg Med Chem Lett. 2013 Jan 1;23(1):273-80. doi: 10.1016/j.bmcl.2012.10.099.
Ahmed Kamal 1,  Jaki R Tamboli,  M V P S Vishnuvardhan,  S F Adil,  V Lakshma Nayak,  S Ramakrishna
Affiliations

Affiliation

  • 1 Division of Organic Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India. ahmedkamal@iict.res.in
PMID: 23182091 DOI: 10.1016/j.bmcl.2012.10.099
Abstract

A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates (16a-i, 17a-i and 18a-d) were synthesized and evaluated for Anticancer activity against five human Cancer cell lines. Among the series, one of the compound 17g showed significant antiproliferative activity in A549 (lung Cancer) cell line. Flow cytometric analysis showed that 17g arrested the cell cycle in the G2/M phase leading to Caspase-3 dependent apoptotic cell death. Further, Hoechst 33258 staining and DNA fragmentation assay also suggests that 17g induces cell death by Apoptosis.

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