Synthesis of 4β-N-polyaromatic substituted podophyllotoxins: DNA topoisomerase inhibition, anticancer and apoptosis-inducing activities

Ahmed Kamal; B Ashwini Kumar; Paidakula Suresh; Satyam Kumar Agrawal; Gousia Chashoo; Shashank K Singh; A K Saxena

doi:10.1016/j.bmc.2010.10.042

Synthesis of 4β-N-polyaromatic substituted podophyllotoxins: DNA topoisomerase inhibition, anticancer and apoptosis-inducing activities

Bioorg Med Chem. 2010 Dec 15;18(24):8493-500. doi: 10.1016/j.bmc.2010.10.042. Epub 2010 Nov 10.

Authors

Ahmed Kamal¹, B Ashwini Kumar, Paidakula Suresh, Satyam Kumar Agrawal, Gousia Chashoo, Shashank K Singh, A K Saxena

Affiliation

¹ Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 607, India. ahmedkamal@iict.res.in

PMID: 21074444
DOI: 10.1016/j.bmc.2010.10.042

Abstract

A new class of 4β-N-polyaromatic substituted podophyllotoxin congeners have been synthesized and evaluated for their DNA topoisomerase-II (topo-II) inhibition as well as anticancer potential in some human cancer cell lines. The ease of synthesis and interesting biological activities make the present series of polyaromatic-podophyllotoxin congeners as a promising new structure for the development of new anticancer agents based on podophyllotoxin scaffold.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects*
Cell Line, Tumor
DNA Topoisomerases, Type II / drug effects*
Drug Screening Assays, Antitumor
Humans
Podophyllotoxin / chemical synthesis*
Podophyllotoxin / pharmacology
Topoisomerase II Inhibitors / chemical synthesis*
Topoisomerase II Inhibitors / pharmacology

Substances

Antineoplastic Agents
Topoisomerase II Inhibitors
DNA Topoisomerases, Type II
Podophyllotoxin