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RESEARCH PRODUCT
Synthesis of novel xanthone and acridone carboxamides with potent antiproliferative activities
Aikaterini F. GiannopoulouKaterina GiotiRoxane TentaNicole PouliDimitrios J. StravopodisSami HamdounAmalia D. KalampalikiAntonios GeorgakopoulosThomas A. EfferthIoannis K. KostakisPanagiotis Marakossubject
General Chemical Engineering02 engineering and technologyAntiproliferative activityXanthone010402 general chemistry01 natural sciencesCell cycle arrestlcsh:Chemistrychemistry.chemical_compoundProstate cancerAcute lymphocytic leukemiaXanthonemedicineAutophagyAcridoneAutophagyGeneral Chemistry021001 nanoscience & nanotechnologymedicine.disease0104 chemical sciencesAcridonechemistrylcsh:QD1-999Cell cultureApoptosisCancer researchNitro0210 nano-technologydescription
Abstract Several new amino-substituted acridone and xanthone derivatives have been designed and synthesized, using an efficient methodology from suitable acridone- or xanthone-carboxylic acid intermediates. The antiproliferative activity of the target compounds has been evaluated against four cancer cell lines, namely breast adenocarcinoma MCF-7, acute lymphocytic leukemia CCRF-CEM, and its doxorubicin-resistant variant CEM/ADR5000 and prostate cancer PC-3 cell lines. Selected derivatives have also been tested against the urinary bladder T24 and metastatic melanoma WM266-4 cancer cell lines. Two nitro substituted acridones, bearing a basic side chain as well, were endowed with a remarkable profile against the majority of the cell lines tested, with IC50 values in the low micromolar range. Both compounds cause accumulation at G0/G1 phase, induce apoptosis, and act as potent autophagy inhibitors in PC-3 cells, suggesting their further evaluation in various pathophysiological environments, conditions, and regimens.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2020-11-01 | Arabian Journal of Chemistry |