91619-33-9Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
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Paragraph 0324, (2021/01/23)
Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Design, synthesis and biological evaluation of new thalidomide analogues as TNF-α and IL-6 production inhibitors
Chaulet, Charlotte,Croix, Cécile,Alagille, David,Normand, Sylvain,Delwail, Adriana,Favot, Laure,Lecron, Jean-Claude,Viaud-Massuard, Marie-Claude
scheme or table, p. 1019 - 1022 (2011/03/21)
Several thalidomide analogues were synthesized and compared to thalidomide and its more active analogue, lenalidomide, for their ability to inhibit the production of the pro-inflammatory cytokine tumour necrosis factor (TNF)-α and interleukin (IL)-6 by LPS-activated peripheral blood mononuclear cells (PBMCs). Among these compounds, two analogues containing sulfonyl group displayed interesting downregulation of TNF-α and IL-6 production.
Exploration of secondary and tertiary pharmacophores in unsymmetrical N,N′-diaryl urea inhibitors of soluble epoxide hydrolase
Anandan, Sampath-Kumar,Gless, Richard D.
scheme or table, p. 2740 - 2744 (2010/07/15)
The impact of various secondary and tertiary pharmacophores on in vitro potency of soluble epoxide hydrolase (sEH) inhibitors based on the unsymmetrical urea scaffold 1 is discussed. N,N′-Diaryl urea inhibitors of soluble epoxide hydrolase exhibit subtle variations in inhibitory potency depending on the secondary pharmacophore but tolerate considerable structural variation in the second linker/tertiary pharmacophore fragment.
Synthesis and anticandidal activity of azole-containing sulfonamides
Qandil, Amjad M.,Hassan, Mohammad A.,Al-Shar'i, Nizar A.
experimental part, p. 99 - 112 (2009/04/03)
Twenty five benzenesulfonamides containing one imidazole or triazole ring, or two imidazole or triazole rings have been synthesized and evaluated as anticandidal agents. The most active compounds were 5c, 6b, 6c, 6e, and 17b, which exhibited MIC values of 4.55-24.39 mM depending on the clinical isolate. Comparing imidazole to triazole derivatives did not show a clear effect on activity. Compounds containing a N-benzyl group also showed no clear evidence on activity given the fact that they have an extra aromatic ring. Secondary sulfonamides, 5l, 5m, and 5n showed activities that were proportional to their lipophilicity. The activities of N-aryl-substituted derivatives 5j, 5k, 5l, 5m, 5n, and 6j were also proportional to their lipophilicity. Halogenation enhanced the activity as a result of improvement of lipophilicity. The presence of two imidazole or triazole rings in the same compound did not show a clear enhancement of activity.
SUBSTITUTED 2-ARYLMETHYLENE-N-ARYL-N'-ARYL-MALONAMIDES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS
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Page/Page column 93, (2008/06/13)
The present invention is directed to substituted 2-arylmethylene-N-aryl-N'-aryl-malonamides and analogs thereof. The present invention also relates to the discovery that the compounds are activators of caspases and inducers of apoptosis. Therefore, the activators os caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of anormal cells occurs.
DIAMINO-PYRIMIDINES AND THEIR USE AS ANGIOGENESIS INHIBITORS
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Page/Page column 111, (2010/02/07)
Benzimidazole derivatives of formula (I) , which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatme
