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Cytotoxic and Antifungal Activity of Arylidene Derivatives of 2, 6-Diphenyl Piperidin-4-one

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Author(s): Rahul L. Jadhav*1 Chandrakant S. Magdum2

Journal: Journal of Pharmacy Research
ISSN 0974-6943

Volume: 4;
Issue: 9;
Start page: 3093;
Date: 2011;
Original page

Keywords: 4-piperidones | cytotoxic agents | a | ß-unsaturated ketones | antifungal agents & Claisen- Schmidt reaction.

ABSTRACT
Various 3, 5 bis (arylidene) 2, 6-diphenyl piperidin-4-one have been synthesized by Claisen Schmidt reaction and characterized by spectral data. These compoundshaving 1, 5-diary -3-oxo-1, 4- pentadinenyl pharmacophore which is considered to interact at a complimentary binding site in susceptible neoplasm and showscytotoxic activity. These compounds interact with cellular thiols and no or little affinity to hydroxy and amino group found in nucleic acid, hence free fromgenotoxic effect. The resulting compounds also possess antifungal activity due to presence of a, ß-unsaturated carbonyl group. The title compounds were preparedby reacting 2, 6-diphenyl piperidin-4-one with aromatic aldehyde derivatives in the basic medium. The synthesized compounds have been screened for cytotoxicproperty by SRB assay at four different concentrations against colon and leukemic cell lines. The compounds 7 showed significant activity against human leukemiacell lines whereas compound 5 showed significant activity against fungal strains of C. albicans. This study revealed the potential of these molecules for furtherdevelopment as cytotoxic and antifungal agents.

Tango Jona
Tangokurs Rapperswil-Jona

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