1174997-03-5Relevant academic research and scientific papers
Sorafenib derivatives induce apoptosis through inhibition of STAT3 independent of Raf
Chen, Kuen-Feng,Tai, Wei-Tien,Huang, Jui-Wen,Hsu, Cheng-Yi,Chen, Wei-Lin,Cheng, Ann-Lii,Chen, Pei-Jer,Shiau, Chung-Wai
scheme or table, p. 2845 - 2851 (2011/07/08)
STAT3 is a transcription factor that modulates survival-directed transcription. It is persistently activated in many human cancers. Literature has shown that sorafenib, Raf kinase inhibitor, reduces Phospho-STAT3 and induces cell death. A series of sorafenib derivatives were synthesized as new inhibitors for STAT3. Urea, sulfonamide, and carboxamide linkers brought out different SARs from the end of sorafenib. Urea and carboxamide linked derivatives showed greater inhibition against STAT3 activity than sulfonamide linked derivatives. In particular, 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(4- (4-cyanophenoxy)phenyl)urea (1), a urea linker, was as potent as sorafenib in reducing P-STAT3 level and cell death but no inhibition for Raf activity. Such result provides a new lead for the design of STAT3 inhibitors.
AMINOQUINOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 6, (2010/10/19)
Provided are a novel aminoquinoline compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, preparation method thereof, and a pharmaceutical composition for preventing or treating cutaneous cancer, comprising the aminoquinoline co
Aminoquinoline derivatives with antiproliferative activity against melanoma cell line
Nam, Bong Soo,Kim, Hwan,Oh, Chang-Hyun,Lee, So Ha,Cho, Seung Joo,Sim, Tae Bo,Hah, Jung-Mi,Kim, Dong Jin,Choi, Jung Hoon,Yoo, Kyung Ho
scheme or table, p. 3517 - 3520 (2010/04/26)
The synthesis of a novel series of aminoquinoline derivatives 1a-p and their antiproliferative activities against A375 human melanoma cell line were described. Most compounds showed superior antiproliferative activities to Sorafenib as a reference compoun
