New derivatives of phaeosphaeride A (PPA) were synthesized and characterized. Anti-tumor activity studies were carried out on the HCT-116, PC3, MCF-7, A549, К562, NCI-Н929, Jurkat, THP-1, RPMI8228 tumor cell lines, and on the HEF cell line. All of the compounds synthesized were found to have better efficacy than PPA towards the tumor cell lines mentioned. Compound was potent against six cancer cell lines, HCT-116, PC-3, K562, NCI-H929, Jurkat, and RPMI8226, showing a 47, 13.5, 16, 4, 1.5, and 7-fold increase in anticancer activity comparative to those of etoposide, respectively. Compound possessed selectivity toward the NCI-H929 cell line (IC = 1.35 ± 0.69 μM), while product was selective against three cancer cell lines, HCT-116, MCF-7, and NCI-H929, each having IC values of 1.65 μM, 1.80 μM and 2.00 μM, respectively.
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| http://dx.doi.org/10.3390/molecules23113043 | DOI Listing |
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