74415-21-7Relevant academic research and scientific papers
Pyrimidine type antitumor compounds having 1,3,4-oxadiazole structure and preparation method and application thereof
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Paragraph 0037; 0043-0044, (2018/12/02)
The invention belongs to the technical field of medicines, relates to compounds having antitumor activity and having specific chemical structures, and particularly relates to pyrimidine type antitumorcompounds having a 1,3,4-oxadiazole structure and a preparation method and application thereof. The general structure formula of the pyrimidine type antitumor compounds is shown as follows in the description. The novel compounds greatly improve antitumor effects, and have more excellent anti-proliferation capability for human lung cancer A549 cells when compared with pyrimidine acylhydrazine compounds. Synthetic steps are simplified in a synthesis process, thus making future industrial production possible.
Design, synthesis and biological activity evaluation of 2,5-diphenyl-1,3,4-oxadiazole derivatives as novel inhibitors of fructose-1,6-bisphosphatase
He, Hai-Bing,Gao, Li-Xin,Zhou, Yue-Yang,Liu, Ting,Tang, Jie,Gong, Xue-Ping,Qiu, Wen-Wei,Li, Jing-Ya,Li, Jia,Yang, Fan
, p. 2693 - 2712 (2013/01/15)
Fructose-1,6-bisphosphatase (FBPase), an important gluconeogenic enzyme, catalyzes the hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate. The effort to discover new FBPase inhibitors was carried out by high-throughput screening (HTS) of a library of 56,000 lead-like compounds, and a 2,5-diphenyl-1,3,4-oxadiazole (3a, IC50 = 15.45 μM) which bearing no phosphate group was identified as a potential FBPase inhibitor for the first time. Structure-activity-relationship (SAR) research of a series of analogues obtained by modifying the substituent groups and replacing the 1,3,4-oxadiazole with several other heterocycles disclosed the key structure and substituent groups related to the binding with FBPase.
Substitution Reactions of Phenylated Aza-heterocycles. Part 1. Nitration of 2,5-Diphenyl-1,3,4-oxadiazole: a Product Study using High Performance Liquid Chromatography
Blackhall, Alexander,Brydon, Donald L.,Saga, Anthony J. G.,Smith, David M.
, p. 773 - 777 (2007/10/02)
Contrary to a previous literature report, nitration of 2,5-diphenyl-1,3,4-oxadiazole (1) under various conditions gives a mixture of all six possible 2,5-bisnitrophenyl derivatives, which may be analysed quantitatively using high performance liquid chromatography.Nitration using nitric acid alone gives mainly the three isomers with p-nitrophenyl groups, i.e. (7), (9), and (10), whereas mixed acids and nitronium tetrafluoroborate give mainly meta-nitration products, i.e. (6), (8), and (9).Nitration of the three 2-(nitrophenyl)-5-phenyl-1,3,4-oxadiazoles also shows considerable variation of product ratio according to the conditions.
