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Antitumor and antileishmanial evaluation of novel heterocycles derived from quinazoline scaffold: a molecular modeling approach

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Abstract

Novel thiazole, pyrimidine and benzylidene derivatives derived from quinazoline scaffold have been synthesized. The antitumor evaluation of the newly synthesized products against three cancer cell lines namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460), and CNS cancer (SF-268) showed that the benzylidene–quinazoline derivative 12a showed remarkable activity against all three cell lines. The thiazolo-quinazoline derivative 10 showed greater activity than the control against breast adenocarcinoma (MCF-7) with a concentration of 0.01 μM. Moreover, the antileishmanial activity of the newly synthesized products tested on Leishmania donovani amastigotes showed that compounds 4, 14, and 18 had very promising activity.

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Acknowledgments

The authors would like to extend their gratitude to the American University in Cairo for its continuous support through funding this research project.

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Authors and Affiliations

  1. Department of Chemistry, American University in Cairo, P.O. Box 74, New Cairo, 11835, Arab Republic of Egypt

    Daisy H. Fleita & Ola K. Sakka

  2. Department of Chemistry, Faculty of Science, Cairo University, Giza, Arab Republic of Egypt

    Rafat M. Mohareb

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  1. Daisy H. Fleita
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  2. Rafat M. Mohareb
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  3. Ola K. Sakka
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Correspondence to Rafat M. Mohareb.

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Fleita, D.H., Mohareb, R.M. & Sakka, O.K. Antitumor and antileishmanial evaluation of novel heterocycles derived from quinazoline scaffold: a molecular modeling approach. Med Chem Res 22, 2207–2221 (2013). https://doi.org/10.1007/s00044-012-0213-9

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