| Literature DB >> 30447888 |
Victoria V Abzianidze1, Sofya A Zakharenkova2, Natalia I Moiseeva3, Petr P Beltyukov4, Valeriy A Polukeev5, Yaroslav A Dubrovskii6, Victor A Kuznetsov4, Yuri G Trishin2, Jennifer E Mejia7, Alvin A Holder8.
Abstract
New derivatives of phaeosphaeride A (PPA) were synthesized and characterized. Anti-tumor studies were carried out on the U937, HCT-116, PC3, MCF-7, A549, К562, NCI-H929, Jurkat, THP-1, RPMI8228 tumor cell lines, and on the HEF cell line. All the compounds synthesized were found to have better efficacy than PPA towards the tumor cell lines mentioned. Compound 6 (IC50 = 0.59 ± 0.27 µM) was observed to be 11 times more active than PPA (IC50 = 6.5 ± 0.30 µM) towards the NCI-H929 cell line, with a therapeutic index of 18. Compound 6 was determined to be over half and 16 times more active than etoposide towards the NCI-H929 (IC50 = 0.9 ± 0.05 µM) and A549 (IC50 = 100 ± 7.0 µM) cell lines, respectively.Entities:
Keywords: Anti-cancer agents; Etoposide; HCT-116 cell line; HEF cell line; In vitro studies; Mercapto derivative; Natural products; Phaeosphaeride A; Therapeutic index
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Year: 2018 PMID： 30447888 DOI： 10.1016/j.bmcl.2018.11.003
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823