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

Abid Hussain Banday, Vinod V. Kulkarni, Victor J Hruby

Research output: Contribution to journalArticle

17 Citations (Scopus)

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. This journal is

Original languageEnglish (US)
Pages (from-to)94-104
Number of pages11
JournalMedChemComm
Volume6
Issue number1
DOIs
StatePublished - Jan 1 2015

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Podophyllotoxin
Chalcone
Cytotoxicity
Antineoplastic Agents
Cells
Click Chemistry
Topoisomerase II Inhibitors
Cell Line
Type II DNA Topoisomerase
Biological Availability
Inhibitory Concentration 50
Molecules
Neoplasms
Proteins
Lead
In Vitro Techniques

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

Cite this

Design, synthesis, and biological and docking studies of novel epipodophyllotoxin-chalcone hybrids as potential anticancer agents. / Banday, Abid Hussain; Kulkarni, Vinod V.; Hruby, Victor J.

In: MedChemComm, Vol. 6, No. 1, 01.01.2015, p. 94-104.

Research output: Contribution to journalArticle

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