1310739-63-9Relevant articles and documents
Design and synthesis of 2-iminothiazolidin-4-one moiety-containing compounds as potent antiproliferative agents
Zhai, Xin,Li, Wei,Chen, Dong,Lai, Ruiwei,Liu, Jun,Gong, Ping
, p. 360 - 367 (2012/07/17)
A new series of 2,5-diaryliminothiazolidin-4-ones were designed and synthesized as potent antiproliferative agents. The antiproliferative activities of the 25 target compounds were evaluated against three cancer cell lines (A549, H460 and HT29) by MTT assay. Pharmacological data indicated that most of the compounds possessed moderate activity, some showed remarkable activity against one or more cell lines. As the most promising compound, 8s (with IC 50 values of 1.1, 0.01 and 1.3μM against the A549, H460 and HT29 cell lines) was 1.1- to 270-fold more potent than the reference drug sorafenib. Furthermore, preliminary structure-activity relationships (SARs) were summarized to provide guidance for further design and discovery of 2-iminothiazolidin-4- one-based antiproliferative agents. A new series of 2,5-diaryliminothiazolidin- 4-ones were designed and synthesized as potent antiproliferative agents. The antiproliferative activities of the 25 target compounds were evaluated against three cancer cell lines (A549, H460 and HT29) by MTT assay. The most promising compound, 8s, was 1.1-270-fold more potent than the reference drug sorafenib. Preliminary structure-activity relationship data provide guidance for further design and discovery of 2-iminothiazolidin-4-one-based antiproliferative agents. Copyright