期刊
ARCHIV DER PHARMAZIE
卷 345, 期 5, 页码 360-367出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201100064
关键词
2-Iminothiazolidin-4-one moiety; Antiproliferative evaluation; Design; Synthesis
资金
- National Natural Science Foundation of China [21002065]
- National S & T Major Project [2009ZX09301-012]
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 IC50 values of 1.1, 0.01 and 1.3?mu M against the A549, H460 and HT29 cell lines) was 1.1- to 270-fold more potent than the reference drug sorafenib. Furthermore, preliminary structureactivity relationships (SARs) were summarized to provide guidance for further design and discovery of 2-iminothiazolidin-4-one-based antiproliferative agents.
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