Synthesis, characterization and in vitro anti-invasive activity screening of polyphenolic and heterocyclic compounds

Parmar, Virinder S. and Sharma, Nawal K. and Husain, Mofazzal and Watterson, Arthur C. and Kumar, Jayant and Samuelson, Lynne A. and Cholli, Ashok L. and Prasad, Ashok K. and Kumar, Ajay and Malhotra, Sanjay and Kumar, Naresh and Jha, Amitabh and Singh, Amarjit and Singh, Ishwar and Himanshu, and Vats, Archana and Shakil, Najam A. and Trikha, Smriti and Mukherjee, Shubasish and Sharma, Sunil K. and Singh, Sanjay K. and Kumar, Ajay and Jha, Hriday N. and Olsen, Carl E. and Stove, Chrisophe P. and Bracke, Marc E. and Mareel, Marc M. (2003) Synthesis, characterization and in vitro anti-invasive activity screening of polyphenolic and heterocyclic compounds. Bioorganic and Medicinal Chemistry, 11 (6). pp. 913-929. ISSN 0968-0896

Full content URL: http://dx.doi.org/10.1016/S0968-0896(02)00539-4

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Item Type:Article
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Abstract

Invasion is the hallmark of malignant tumors, and is responsible for the bad prognosis of the untreated cancer patients. The search for anti-invasive treatments led us to screen compounds of different classes for their effect in an assay for invasion. Thirty-nine new compounds synthesized in the present study along with 56 already reported compounds belonging mainly to the classes of lactones, pyrazoles, isoxazoles, coumarins, desoxybenzoins, aromatic ketones, chalcones, chromans, isoflavanones have been tested against organotypic confronting cultures of invasive human MCF-7/6 mammary carcinoma cells with embryonic chick heart fragments in vitro. Three of them (a pyrazole derivative, an isoxazolylcoumarin and a prenylated desoxybenzoin) inhibited invasion at concentrations as low as 1 muM; instead of occupying and replacing the heart tissue within 8 days, the MCF-7/6 cells grew around the heart fragments and left it intact, when treated with these compounds. At the anti-invasive concentration of 1 muM, the three compounds did not affect the growth of the MCF-7/6 cells, as shown in the sulforhodamine B assay. Aggregate formation on agar was not stimulated by any of the three anti-invasive compounds, making an effect on the E-cadherin/catenin complex improbable. This is an invasion suppressor that can be activated in MCF-7/6 cells by a number of other molecules. Our data indicate that some polyphenolic and heterocyclic compounds are anti-invasive without being cytotoxic for the cancer cells. (C) 2003 Elsevier Science Ltd. All rights reserved.

Keywords:Pharmacy
Subjects:B Subjects allied to Medicine > B200 Pharmacology, Toxicology and Pharmacy
Divisions:College of Science > School of Pharmacy
ID Code:11307
Deposited On:24 Jul 2013 08:43

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