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Novel 2,4- thiazolidinediones: Synthesis, in vitro cytotoxic activity, and mechanistic investigation.

Abstract：

:Two thiazolidinedione scaffolds different in the position of the thiazolidinedione ring in the molecule were tested for in vitro cytotoxic activity in a panel of human cancer cell lines namely, prostate cancer cells PC-3, breast carcinoma cells MDA-MB-231, and fibrosarcoma cells HT-1080. Some of the target compounds of the A-series where the thiazolidinedione ring is terminal, displayed cytotoxic activity in the low micromolar range in the cell lines tested. Target thiazolidinediones of the B-series where the thiazolidinedione ring is located in the middle of the molecule showed cytotoxic activity comparable to that of their A-series counterparts. Our mechanistic studies indicated that the most cytotoxic compounds in this study have pro-apoptotic capacity. Key signaling mechanisms were investigated and found to vary depending on the target cell context, in line with previous observations regarding thiazolidinediones.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Metwally K,Pratsinis H,Kletsas D

doi

10.1016/j.ejmech.2017.03.052

subject

Has Abstract

pub_date

2017-06-16 00:00:00

pages

340-350

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30219-2

journal_volume

133

pub_type

杂志文章

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