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Novel Biginelli dihydropyrimidines with potential anticancer activity: A parallel synthesis and CoMSIA study

Kumar, BR Prashantha and Sankar, Gopu and Baig, RB Nasir and Chandrashekaran, Srinivasan (2009) Novel Biginelli dihydropyrimidines with potential anticancer activity: A parallel synthesis and CoMSIA study. In: European Journal of Medicinal Chemistry, 44 (10). pp. 4192-4198.

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Novel Biginelli dihydropyrimidines of biological interest were prepared using p-toluene sulphonic acid as an efficient catalyst. All the thirty-two synthesised dihydropyrimidines were evaluated for their in vitro antioxidant activity using DPPH method. Only, compounds 28 and 29 exhibited reasonably good antioxidant activity. Furthermore, the synthesised Biginelli compounds were subjected for their in vitro anticancer activity against MCF-7 human breast cancer cells. The title compounds were tested at the concentration of 10 μg. Compounds exhibited activity ranging from weak to moderate and, from moderate to high in terms of percentage cytotoxicity. Among them, compounds 10 and 11 exhibited significant anticancer activity. In order to elucidate the three-dimensional structure–activity relationships (3D QSAR) towards their anticancer activity, we subjected them for comparative molecular similarity indices analysis (CoMSIA). Illustration regarding their synthesis, analysis, antioxidant activity, anticancer activity and 3D QSAR study is described.

Item Type: Journal Article
Additional Information: Copyright of this article belongs to Elsevier Science.
Keywords: Biginelli dihydropyrimidines;Anticancer activity;MCF-7 cells; CoMSIA;3D QSAR.
Department/Centre: Division of Chemical Sciences > Organic Chemistry
Depositing User: Id for Latest eprints
Date Deposited: 21 Dec 2009 06:42
Last Modified: 16 Dec 2010 09:49
URI: http://eprints.iisc.ac.in/id/eprint/23279

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