- Design and synthesis of novel imidazo[4,5-b]pyridine based compounds as potent anticancer agents with CDK9 inhibitory activity
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New imidazo[4,5-b]pyridine derivatives were designed, synthesized and screened for their anticancer activity against breast (MCF-7) and colon (HCT116) cancer cell lines. Nine compounds (I, II, IIIa, IIIb, IV, VI, VIIa, VIII, IX) showed significant activit
- Ghanem, Nada M.,Farouk, Faten,George, Riham F.,Abbas, Safinaz E.S.,El-Badry, Ossama M.
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- N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
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Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat neurological diseases. In search of new FAAH inhibitors, we identified 2-(4-cyclohexylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4g, with an IC50 of 2.6 μM as a chemical starting point for the development of potent FAAH inhibitors. Preliminary hit-to-lead optimisation resulted in 2-(4-phenylphenoxy)-N-(3-(oxazolo[4,5-b]pyridin-2-yl)phenyl)acetamide, 4i, with an IC50 of 0.35 μM.
- Sunduru, Naresh,Svensson, Mona,Cipriano, Mariateresa,Marwaha, Sania,Andersson, C. David,Svensson, Richard,Fowler, Christopher J.,Elofsson, Mikael
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p. 513 - 521
(2017/11/10)
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- 1-[4-(1H-Benzoimidazol-2-yl)-phenyl]-3-[4-(1H-benzoimidazol-2-yl)-phenyl] -urea derivatives as small molecule heparanase inhibitors
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A novel class of 1-[4-(1H-benzoimidazol-2-yl)-phenyl]-3-[4-(1H- benzoimidazol-2-yl)-phenyl]-ureas are described as potent inhibitors of heparanase. Among them are 1,3-bis-[4-(1H-benzoimidazol-2-yl)-phenyl]-urea (7a) and 1,3-bis-[4-(5,6-dimethyl-1H-benzoimidazol-2-yl)-phenyl]-urea (7d), which displayed good heparanase inhibitory activity (IC50 0.075-0.27 μM). Compound 7a showed good efficacy in a B16 metastasis model.
- Pan, Weitao,Miao, Hua-Quan,Xu, Yong-Jiang,Navarro, Elizabeth C.,Tonra, James R.,Corcoran, Erik,Lahiji, Armin,Kussie, Paul,Kiselyov, Alexander S.,Wong, Wai C.,Liu, Hu
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p. 409 - 412
(2007/10/03)
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- Carbon-13 NMR Spectra of Isomeric 2-Arylimidazopyridines
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The 13C NMR spectra of some 2-arylimidazo-- and -pyridines and their protonated forms have been studied.The nitrogen atom of the pyridine ring has been shown to be the most basic nitrogen in these compounds.
- Tretyakov, A. V.,Rudaya, L. I.,El'tsov, A. V.,Larin, M. F.,Lopyrev, V. A.
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