Issue 1, 2015

Design, synthesis, and biological and docking studies of novel epipodophyllotoxin–chalcone hybrids as potential anticancer agents

Abstract

A series of new compounds consisting of epipodophyllotoxin–chalcone hybrids was synthesized towards the development of better anticancer lead molecules. These hybrids consist of structurally different but functionally similar topoisomerase-II inhibitors which were conjugated together through click-chemistry. Their design is aimed at the synthesis of novel chemotherapeutics with a better target-protein interaction and higher bioavailability. Evaluation of the anticancer activity of these designed conjugates against a panel of six human cancer cell lines proved their potential cytotoxicity. Further, these compounds were docked against topoisomerase-II and the energy calculations were in good agreement with the observed IC50 values. Compounds 6d, 6f, 7d and 7f exhibited significant in vitro cytotoxicity. Among all the compounds evaluated, compound 7f was found to be the most promising, especially selective against SW-620 and SKN-SH cell lines.

Graphical abstract: Design, synthesis, and biological and docking studies of novel epipodophyllotoxin–chalcone hybrids as potential anticancer agents

Supplementary files

Article information

Article type
Concise Article
Submitted
27 Jul 2014
Accepted
08 Sep 2014
First published
11 Sep 2014

Med. Chem. Commun., 2015,6, 94-104

Design, synthesis, and biological and docking studies of novel epipodophyllotoxin–chalcone hybrids as potential anticancer agents

A. H. Banday, V. V. Kulkarni and V. J. Hruby, Med. Chem. Commun., 2015, 6, 94 DOI: 10.1039/C4MD00325J

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