22952-19-8Relevant academic research and scientific papers
N,N'-bis-substituted aryl thiourea derivatives and synthetic method and application thereof
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Paragraph 0056; 0058; 0065; 0066, (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.
Structure-based design and synthesis of novel pseudosaccharine derivatives as antiproliferative agents and kinase inhibitors
Elsayed, Mohamed S.A.,El-Araby, Moustafa E.,Serya, Rabah A.T.,El-Khatib, Ahmed H.,Linscheid, Michael W.,Abouzid, Khaled A.M.
, p. 122 - 131 (2013/04/23)
This study is concerned with the implementation of structure-based techniques for the design of new heterocyclic compounds based on pseudosaccharine scaffold with protein kinase inhibition activity. This nucleus was exploited based on the well-known quinazoline core and its interactions with several protein kinases. Two series of compounds employing this new scaffold were synthesized and evaluated at enzymatic and cellular levels. Compound 9b displayed broad spectrum antiproliferative activity on NCI 60-cell lines panel with mean GI50 of 5.4 μM. Investigation of the molecular mechanism showed probable inhibitory activity against Src kinase.
