1.
Bioorg Med Chem Lett
; 29(1): 59-61, 2019 01 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-30447888
RESUMEN
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, Ð562, 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 (IC50â¯=â¯0.59⯱â¯0.27⯵M) was observed to be 11 times more active than PPA (IC50â¯=â¯6.5⯱â¯0.30⯵M) 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 (IC50â¯=â¯0.9⯱â¯0.05⯵M) and A549 (IC50â¯=â¯100⯱â¯7.0⯵M) cell lines, respectively.