42340-98-7Relevant articles and documents
Blockade of STAT3 activation by sorafenib derivatives through enhancing SHP-1 phosphatase activity
Hsu, Cheng-Yi,Liu, Chun-Yu,Shiau, Chung-Wai,Chen, Kuen-Feng,Chen, Pei-Jer,Tai, Wei-Tien,Huang, Jui-Wen,Kim, Inki
, p. 220 - 227,8 (2020/07/31)
Previously, we demonstrated that the multiple kinase inhibitor sorafenib mediates the repression of phospho-STAT3 in hepatocellular carcinoma cells. In this study, we used this kinase-independent mechanism as a molecular basis to use sorafenib as scaffold to develop a novel class of SHP-1-activating agents. The proof of principle of this premise was provided by SC-1, which on replacement of N-methylpicolinamide by a phenylcyano group showed abolished kinase activity while retaining phospho-STAT3 repressive activity. Structural optimization of SC-1 led to compound 6, which repressed phospho-STAT3 through SHP-1 activation and inhibited PLC5 cell proliferation at sub-micromolar potency. In light of the pivotal role of phospho-STAT3 in promoting tumorigenesis and drug resistance, this novel SHP-1-activating agent may have therapeutic relevance in cancer therapy.
Cyano-3-phenoxybenzyl N-1-(1-naphthyl) ethylcarbamate
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, (2008/06/13)
Diastereomeric esters of 2-phenylamino-3-methylbutanoic acids, novel intermediates therefor, synthesis thereof, and the use of said esters for the control of pests.
Enantiomerically Pure Lactones. 2. Approaches to Cis or Trans Multicyclic Lactones
Pirkle, William H.,Adams, Paul E.
, p. 4111 - 4117 (2007/10/02)
Enantiomerically pure bicyclic lactones 1-3 and tricyclic lactones 4 and 5 have been prepared by either of two procedures, each hinging upon the liquid chromatographic seperation of rationally selected diastereomeric derivatives.After seperation, the diastereomers are converted by a simple high-yield reaction sequence to the enantiomeric multiring lactones, none of which has been previously reported in optically active form. The relative strengths and weaknesses of each approach are discussed.Lactones 4 and 5 were α-methylated, these derivatives being suitable for the determination of enantiomeric purity and absolute configuration using the chiral solvating agent (S)-(+)-2,2,2-trifluoro-1-(9-anthryl)ethanol.