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Synthesis and Cytotoxic Evaluation for Some New Dihydropyrimidinone Derivatives for Anticancer Activity

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A new combination of reagent (ZnCl2/TBAB) system has been developed for the preparation of dihydropyrimidinones by using aldehyde, acetoacetic ester and urea or thiourea. These improved reaction condition allow the preparation of a wide variety of substituted dihydropyrimidinones in high yields and purity under mild reaction conditions. Some of the dihydropyrimidinones were showed moderate in vitro cytotoxic activity against U937, Colo205, A549 and THP-1 human cancer cell lines. Some of the compounds have been found promising anticancer activity when compared standard drug etoposide.

Keywords: Biginelli reaction; Cytotoxicity; Dihydropyrimidinones; MTT assay; One pot synthesis; ZnCl2/TBAB catalyst

Document Type: Research Article

Publication date: 01 October 2013

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  • Letters in Drug Design & Discovery publishes original letters on all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis will be on publishing quality papers very rapidly. Letters will be processed rapidly by taking full advantage of Internet technology for both the submission and review of manuscripts. The journal is essential reading to all pharmaceutical scientists involved in research in drug design and discovery.
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