1416587-64-8Relevant articles and documents
Identification of anticancer agents based on the thieno[2,3-b]pyridine and 1H-pyrazole molecular scaffolds
Eurtivong, Chatchakorn,Reynisdóttir, Inga,Kuczma, Stephanie,Furkert, Daniel P.,Brimble, Margaret A.,Reynisson, Jóhannes
, p. 3521 - 3526 (2016)
Structural similarity search of commercially available analogues of thieno[2,3-b]pyridine and 1H-pyrazole derivatives, known anticancer agents, resulted in 717 hits. These were docked into the phosphoinositide specific-phospholipase C (PLC) binding pocket, the putative target of the compounds, to further focus the selection. Thirteen derivatives of the thieno[2,3-b]pyridines were identified and tested against the NCI60 panel of human tumour cell lines. The most active derivative 1 was most potent against the MDA-MB-435 melanoma cell line with GI50at 30?nM. Also, it was found that a piperidine moiety is tolerated on the thieno[2,3-b]pyridine scaffold with GI50?=?296?nM (MDA-MB-435) for derivative 10 considerably expanding the structure activity relationship for the series. For the 1H-pyrazoles four derivatives were identified using the in silico approach and additionally ten were synthesised with various substituents on the phenyl moiety to extend the structural activity relationship but only modest anticancer activity was found.
Method for synthesis of substituted 1-sulfonyl-1H-pyrazole
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Paragraph 0047; 0048; 0049; 0050; 0051, (2017/10/07)
The invention discloses a method for synthesis of substituted 1-sulfonyl-1H-pyrazole, and aims to provide a method for synthesis of 1-sulfonyl-1H-pyrazole, the method has the advantages of simple and easily available starting materials, high yield and easy operation, the method is characterized in that sulfonyl hydrazone, N, N-dimethylmalononitrile and a Lewis acid catalyst are in turn added into an organic solvent for heating refluxing reaction to obtain the substituted 1-sulfonyl-1H-pyrazole, and the method belongs to the organic synthesis technical field.