1313803-53-0Relevant articles and documents
Synthesis and cytotoxic evaluation of novel N-methyl-4-phenoxypicolinamide derivatives
Li, Wei,Zhai, Xin,Ding, Lu,Sun, Limin,Chen, Xiaomei,Gong, Ping,Sun, Tiemin
, p. 5130 - 5141 (2011)
A series of N-methyl-4-phenoxypicolinamide derivatives were synthesized and evaluated in vitro for their cytotoxic activity against A549, H460 and HT29 cell lines. Pharmacological data indicated that some of the target compounds possessed marked antiproliferative activity, superior to that of the reference drug sorafenib. As the most promising compound, 8e exhibited potent cytotoxicity with the IC50 value of 3.6, 1.7 and 3.0 μM against A549, H460 and HT-29 cell lines, respectively.
N,N'-bis-substituted aryl thiourea derivatives and synthetic method and application thereof
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, (2017/04/26)
The invention discloses N,N'-bis-substituted aryl thiourea derivatives which are a series of compounds simultaneously containing various substituted aromatic ring structures and asymmetric substituted thiourea structures and are all novel structural compounds which are not reported in the literature. The biological activity test analysis of all the target compounds includes determination of DPPH antioxidant activity and antiviral activity. Results indicate that, in general, the designed and synthesized compounds are novel in structures and have the antioxidant activity and the antiviral activity revealed for the first time. In addition, the unknown biological activity is not fully elucidated, and thus the compounds are expected to provide a certain material basis for further research and development of new drugs.
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