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

Abstract：

: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 microg. 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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Prashantha Kumar BR,Sankar G,Nasir Baig RB,Chandrashekaran S

doi

10.1016/j.ejmech.2009.05.014

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

4192-8

issue

10

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00306-7

journal_volume

44

pub_type

杂志文章

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