Synthesis, antitumor and antibacterial activities of certain substituted pyrimidines bearing benzofuran

V.H. Babu, P.S. Kumar, K.K. Srinivasan, G.V. Bhat

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Benzofuran chalcones (2a-i) were prepared by the reaction of 2-acetylbenzofuran (1) with different aromatic aldehydes in the presence of a strong base. Cyclocondensation of benzofuran chalcones with guanidine hydrochloride, thiourea and urea resulted in the formation of various aminopyrimidines (3a-i), thiopyrimidines (4a-i) and hydroxy pyrimidines (5a-i), respectively. The structures of all the compounds (2,3,4,5 a-i) have been established on the basis of analytical and spectral data. All the compounds have been screened for antitumour and antimicrobial activities. Compounds 3b and 3d showed significant antitumour activity. While compounds 4d and 4h showed only moderate activity against Staphylococcus aureus at 500 μg/ml, compounds 4h, 4i, 5a, 5b, 5h and 5i showed promising activity against Candida albicans at 500 μg/ml concentrations.
Original languageEnglish
Pages (from-to)647-652
Number of pages6
JournalIndian Journal of Pharmaceutical Sciences
Issue number5
Publication statusPublished - 2004


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