6533b7cffe1ef96bd125978f
RESEARCH PRODUCT
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subject
biology010405 organic chemistryStereochemistryPharmaceutical Sciencemedicine.diseasebiology.organism_classification01 natural sciences0104 chemical sciencesMultiple drug resistance03 medical and health sciencesLeukemiaHydrolysisSponge0302 clinical medicineCell culture030220 oncology & carcinogenesisDrug DiscoverymedicineSteglich esterificationCytotoxicityPharmacology Toxicology and Pharmaceutics (miscellaneous)IC50description
The 6-epimer of the plakortide H acid (1), along with the endoperoxides plakortide E (2), plakortin (3), and dihydroplakortin (4) have been isolated from a sample of the Caribbean sponge Plakortis halichondrioides. To perform a comparative study on the cytotoxicity towards the drug-sensitive leukemia CCRF-CEM cell line and its multi-drug resistant subline CEM/ADR5000, the acid of plakortin, namely plakortic acid (5), as well as the esters plakortide E methyl ester (6) and 6-epi-plakortide H (7) were synthesized by hydrolysis and Steglich esterification, respectively. The data obtained showed that the acids (1, 2, 5) exhibited potent cytotoxicity towards both cell lines, whereas the esters showed no activity (6, 7) or weaker activity (3, 4) compared to their corresponding acids. Plakortic acid (5) was the most promising derivative with half maximal inhibitory concentration (IC50) values of ca. 0.20 µM for both cell lines.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2017-03-03 | Marine Drugs |