Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


A Triphenyltin(IV) Nicotinate Derivative – Synthesis and Toxicity Towards Different Tumour and Normal Cell Lines

Author(s): Santiago Gomez-Ruiz, Zeljko Zizak, Goran N. Kaluderovic.


[SnPh3(DMNI)] (1), (2,6-dimethoxynicotinic acid (DMNIH)) was prepared by the reaction of SnPh3Cl with DMNIH. Molecular structure of 1 was determined by X-ray diffraction studies. The cytotoxic activity of 1 was tested against tumour cell lines human cervical adenocarcinoma HeLa, human myelogenous leukemia K562, human malignant melanoma Fem-x and normal immunocompetent cells, non-stimulated peripheral blood mononuclear cells (PBMC-PHA) and with phytohemagglutinin stimulated peripheral blood mononuclear cells (PBMC+PHA) showing a very high antiproliferative activity against tumour cell lines with IC50 values (after 72 h of treatment) in the range of 46–65 nM. This toxicity becomes lower against normal immunocompetent cells (IC50 values in the range of 88–148 nM) indicating some degree of selectivity towards cancer cell lines.

Keywords: Anticancer drugs, Carboxylato ligands, Cytotoxicity, Metal-based drugs, Nicotinato ligands, Tin, phytohemagglutinin, antiproliferative activity, carboxylate derivatives, 2, 6-dimethoxynicotinic acid

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Article Details

Year: 2012
Page: [737 - 741]
Pages: 5
DOI: 10.2174/157018012802652976
Price: $58