4.7 Article

Towards cytotoxic and selective derivatives of maslinic acid

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 1, Pages 594-615

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.10.047

Keywords

Maslinic acid; Esters; Cancer; SRB assay; Antitumor; DNA laddering; Annexin V assay; Cell cycle investigations; Apoptosis; Caspase activity

Funding

  1. Grunderwerkstatt-Biowissenschaften

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Several novel esters and amides of maslinic acid were prepared. Their evaluation for cytotoxic activity with a panel of human cancer cell lines using a sulforhodamine B (SRB) assay revealed for some of them a noteworthy activity. The results from annexinV-FITC and caspase-assays as well as from DNA laddering experiments provided evidence for an apoptotic cell death. A diacetylated benzylamide (15) induced a G1/G0 arrest in tumor cells. It also displayed an extraordinary cytotoxicity against human ovarian cancer cells but a 300 times lower toxicity for non-malignant primary human fibroblasts. (C) 2013 Elsevier Ltd. All rights reserved.

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