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Antiproliferative effect of synthetic cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against human cancer cell lines

  • Dorimar Stiz , Adriana Campos , Ana Lúcia Tasca Gois Ruiz , João Ernesto de Carvalho , Rogério Corrêa and Valdir Cechinel-Filho EMAIL logo
Published/Copyright: October 21, 2016

Abstract

This work describes the antiproliferative potential of 14 cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against several human cancer cell lines. The antiproliferative effect was evaluated using the sulforhodamine B assay. Although some compounds from methylphtalimide and carboxylic acid phtalimide classes exhibited a selective antiproliferative activity, the itaconimides (11–14) exhibited the best results, especially compound 14, which presented a TGI (concentration that produces total growth inhibition) value of 0.0043 μM against glioma (U251), being inactive against the non-tumor cell line (HaCat). Absorption, distribution, metabolism and excretion in silico evaluations suggest that these compounds are promising candidates.

Acknowledgments

The authors are grateful to the National Council for Scientific and Technological Development (Conselho Nacional de Desenvolvimento Científico e Tecnológico – CNPq), Fundo de Apoio à Manutenção e ao Desenvolvimento da Educação Superior – FUMDES (State of Santa Catarina) and RIBECANCER (RT 0464)/CYTED/CNPq Network, for their financial support.

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Received: 2016-4-1
Revised: 2016-9-6
Accepted: 2016-9-20
Published Online: 2016-10-21
Published in Print: 2016-11-1

©2016 Walter de Gruyter GmbH, Berlin/Boston

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