Antiproliferative effect of synthetic cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against human cancer cell lines
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Dorimar Stiz
, Adriana Campos , Ana Lúcia Tasca Gois Ruiz , João Ernesto de Carvalho , Rogério Corrêa and Valdir Cechinel-Filho
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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©2016 Walter de Gruyter GmbH, Berlin/Boston
Articles in the same Issue
- Frontmatter
- Research Articles
- Seasonal variation of gastroprotective terpenoids in Maytenus robusta (Celastraceae) quantified by gas chromatography-flame ionization detection (GC-FID)
- Plicosepalin A, a new antioxidant catechin–gallic acid derivative of inositol from the mistletoe Plicosepalus curviflorus
- New lupan-type triterpenoids
- Penicilloitins A and B, new antimicrobial fatty acid esters from a marine endophytic Penicillium species
- Anti-acetylcholinesterase activity of essential oils and their major constituents from four Ocimum species
- The chemical composition, antimicrobial, and antioxidant activities of Pycnocycla spinosa and Pycnocyla flabellifolia essential oils
- Biological evaluation and docking studies of some benzoxazole derivatives as inhibitors of acetylcholinesterase and butyrylcholinesterase
- LC/ESI-MS/MS profiling of Ulmus parvifolia extracts and evaluation of its anti-inflammatory, cytotoxic, and antioxidant activities
- Antiproliferative effect of synthetic cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against human cancer cell lines
- Anti-inflammatory activity of highly oxygenated terpenoids from Achillea biebersteinii Afan
- Annual Reviewer Acknowledgement
- Reviewer acknowledgement Biosciences – Zeitschrift für Naturforschung C, volume 71 (2016)
Articles in the same Issue
- Frontmatter
- Research Articles
- Seasonal variation of gastroprotective terpenoids in Maytenus robusta (Celastraceae) quantified by gas chromatography-flame ionization detection (GC-FID)
- Plicosepalin A, a new antioxidant catechin–gallic acid derivative of inositol from the mistletoe Plicosepalus curviflorus
- New lupan-type triterpenoids
- Penicilloitins A and B, new antimicrobial fatty acid esters from a marine endophytic Penicillium species
- Anti-acetylcholinesterase activity of essential oils and their major constituents from four Ocimum species
- The chemical composition, antimicrobial, and antioxidant activities of Pycnocycla spinosa and Pycnocyla flabellifolia essential oils
- Biological evaluation and docking studies of some benzoxazole derivatives as inhibitors of acetylcholinesterase and butyrylcholinesterase
- LC/ESI-MS/MS profiling of Ulmus parvifolia extracts and evaluation of its anti-inflammatory, cytotoxic, and antioxidant activities
- Antiproliferative effect of synthetic cyclic imides (methylphtalimides, carboxylic acid phtalimides and itaconimides) against human cancer cell lines
- Anti-inflammatory activity of highly oxygenated terpenoids from Achillea biebersteinii Afan
- Annual Reviewer Acknowledgement
- Reviewer acknowledgement Biosciences – Zeitschrift für Naturforschung C, volume 71 (2016)