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Synthesis and Cytotoxic Evaluation of Some New 4(3H)-Quinazolinones on Hela Cell Line



Khodarahmi GA1 ; Shamshiri M1 ; Hassanzadeh F1
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Research in Pharmaceutical Sciences Published:2012

Abstract

Quinazolinone backbone is present in a large number of bioactive substances. Since remarkable cytotoxic activity is associated with some 4(3H)-quinazolinones, in this study some 4(3H)-quinazolinone were synthesized and screened against HeLa cells. The synthesis was performed via reaction of anthranilic acid with dicarboxylic anhydrides to produce carboxylic acids derivatives. The products were heated in acetic anhydride to produce benzoxazinones. Finally, 4(3H)-quinazolinones were synthesized by reaction between benzoxazinones and primary amines. The assessment of the structure of the synthesized compounds was based on spectral data (FT-IR, Mass and 1HNMR). Subsequently, cytotoxic activity of compounds 3, 6, 9 and 13 (individually and in combination with doxorubicin) was evaluated on HeLa cell line using MTT assay. The results indicated that the tested compounds did not show significant cytotoxicity alone and in combination with doxorubicin (1 and 20 μM).
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