- Structure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKKβ phosphorylation for pancreatic cancer therapy
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Genetic models validated Inhibitor of nuclear factor (NF) kappa B kinase beta (IKKβ) as a therapeutic target for KRAS mutation associated pancreatic cancer. Phosphorylation of the activation loop serine residues (S177, S181) in IKKβ
- Sagar, Satish,Singh, Sarbjit,Mallareddy, Jayapal Reddy,Sonawane, Yogesh A.,Napoleon, John V.,Rana, Sandeep,Contreras, Jacob I.,Rajesh, Christabelle,Ezell, Edward L.,Kizhake, Smitha,Garrison, Jered C.,Radhakrishnan, Prakash,Natarajan, Amarnath
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- Thiazolo[5,4-f]quinoxalines, Oxazolo[5,4-f]quinoxalines and Pyrazino[b,e]isatins: Synthesis from 6-Aminoquinoxalines and Properties
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The regioselective iodination of different 2-mono-, 3-mono- and 2,3-disubstituted 6-aminoquinoxalines, which takes place at their 5-position, was rationalized on the basis of Hückel theory calculations. Oxazolo- and thiazolo[5,4-f]quinoxaline analogues of
- Bach, Stéphane,Dorcet, Vincent,El Osmani, Nour,Erb, William,Fajloun, Ziad,Lassagne, Frédéric,Mongin, Florence,Mongin, Olivier,Picot, Laurent,Richy, Nicolas,Robert, Thomas,Roisnel, Thierry,Sims, Joshua M.,Thiéry, Valérie
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p. 2756 - 2763
(2021/06/25)
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- Design, synthesis and biological evaluation of novel fluorinated heterocyclic hybrid molecules based on triazole & quinoxaline scaffolds lead to highly potent antimalarials and antibacterials
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A series of novel fluorinated heterocyclic hybrid molecules based on triazole & quinoxaline scaffold were designed, synthesized and evaluated for inhibition of Plasmodium falciparum, a virulent human malaria parasite. Mono and bis triazole tagged quinoxal
- Chandra Shekhar, Adimulam,Venkat Lingaiah, Boddupally Pedda,Shanthan Rao, Pamulaparthy,Narsaiah, Banda,Aparna Devi, Allanki,Sijwali, Puran Singh
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p. 393 - 407
(2015/06/22)
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- Emergence of pyrido quinoxalines as new family of antimalarial agents
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A series of novel N-alkyl dihydro pyrido quinoxaline derivatives were synthesized using Gould-Jacobs reaction and evaluated their antimalarial activity in vitro against chloroquine sensitive (3D7) and drug resistant (Dd2) strains of Plasmodium falciparum.
- Chandra Shekhar,Shanthan Rao,Narsaiah,Allanki, Aparna Devi,Sijwali, Puran Singh
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p. 280 - 287
(2014/04/03)
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- A new facile, efficient synthesis and structure peculiarity of quinoxaline derivatives with two benzimidazole fragments
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A highly efficient and versatile method for the synthesis of quinoxaline derivatives with two benzimidazole fragments have been developed on the basis of the ring contraction of 3-(benzimidazo-2-yl)quinoxalin-2(1H)-one with 1,2-diaminobenzene and its various types of substituted and condensed derivatives. Owing to the inter- and intramolecular processes, involving self association, proton exchange, conformational, and/or tautomeric exchanges between several forms for most of the bis-benzimidazolylquinoxalines signals of bridged and neighboring carbon atoms and the hydrogen atoms of the neighboring carbon atoms of benzimidazole fragments in the NMR spectra are broadened. The conjugation between the benzimidazole fragments and the quinoxaline core of the molecules is increased from the quinoxaline derivative (10c) to its thiadiazol[f]- (17) and pyrrolo[a]-(19) annulated derivatives, resulting in a greater planarity of the molecule as a whole.
- Mamedov, Vakhid A.,Zhukova, Nataliya A.,Syakaev, Victor V.,Gubaidullin, Aidar T.,Beschastnova, Tat'Yana N.,Adgamova, Dil'Bar I.,Samigullina, Aida I.,Latypov, Shamil K.
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supporting information
p. 1403 - 1416
(2013/02/23)
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- Perturbing pro-survival proteins using quinoxaline derivatives: A structure-activity relationship study
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In HeLa cells the combinatorial knockdown of Bcl-xL and Mcl-1 is sufficient to induce spontaneous apoptosis. Quinoxaline derivatives were screened for the induction of Mcl-1 dependent apoptosis using a cell line without functional Bcl-xL. Quinoxaline urea
- Rajule, Rajkumar,Bryant, Vashti C.,Lopez, Hernando,Luo, Xu,Natarajan, Amarnath
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p. 2227 - 2234
(2012/06/01)
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- 2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: A structure-activity relationship study
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The quinoxaline core is considered a privileged scaffold as it is found in a variety of biologically relevant molecules. Here we report the synthesis of a quinoxalin-6-amine library, screening against a panel of cancer cell lines and a structure-activity
- Chen, Qianyi,Bryant, Vashti C.,Lopez, Hernando,Kelly, David L.,Luo, Xu,Natarajan, Amarnath
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p. 1929 - 1932
(2011/04/24)
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- Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors
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A series of quinoxalinylurea-based inhibitors are synthesized and shown to be the novel and potent inhibitors against Jnk Stimulatory Phosphatase-1 (JSP-1), which is a special member of dual-specificity protein phosphatase (DSP) family. Biological assay a
- Zhang, Li,Qiu, Beiying,Xiong, Bing,Li, Xin,Li, Jingya,Wang, Xin,Li, Jia,Shen, Jingkang
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p. 2118 - 2122
(2008/02/01)
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- Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines
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A series of 29 new quinoxalines was synthesized and evaluated in vitro against several parasites (Leishmania donovani, Trypanosoma brucei brucei, and Trichomonas vaginalis). Several of them displayed interesting activities, and particularly four quinoxaline amides showed in vitro antileishmanial properties (IC50 less than 20 μM).
- Hui, Xu,Desrivot, Julie,Bories, Christian,Loiseau, Philippe M.,Franck, Xavier,Hocquemiller, Reynald,Figadere, Bruno
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p. 815 - 820
(2007/10/03)
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- General microwave-assisted protocols for the expedient synthesis of quinoxalines and heterocyclic pyrazines
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Functionalized quinoxalines and heterocyclic pyrazines are expediently prepared in excellent yields (69-99%) from common 1,2-diketone intermediates under microwave irradiation. In addition to being general for a variety of aryl/heteroaryl 1,2-diamines and
- Zhao, Zhijian,Wisnoski, David D.,Wolkenberg, Scott E.,Leister, William H.,Wang, Yi,Lindsley, Craig W.
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p. 4873 - 4876
(2007/10/03)
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- Spectral-luminescent properties of 2,3-diphenyl-6-X-quinoxalines
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A study is made of the spectral-luminescent properties of solutions of 2- and 6-phenylquinoxalines and 2,3-diphenyl-6-X-quinoxalines (X = H, CH3, OC2H5, NH2, C6H5, C6H5O, C6H5CHOH, I, Br, Cl) in a hydrocarbon and 95% ethanol at 295 and 77 K. The energies of the S1 and T1 states obtained (25 600-27 700 and 18 500-20 000 cm-1, respectively) are correlated to the nature of the substituents. The mixed character of the luminescence is inferred from the close location of the S(ππ*) and S(nπ*) levels for the majority of the compounds. The contribution from the ππ* component increases with increasing electron-donating power of the substituent, as well as in going from nonpolar to polar solvent. The quantum yields of fluorescence φ = 10-4-1.1 × 10-1, of the intercombination transition φST = 0.3-0.9, and of phosphorescence φph = 0.2-0.9, the phosphorescence lifetime (τph = 10-3-0.57 s), as well as the established phenomenon of phosphorescence of liquid solutions, are analyzed in the framework of the vibronic and spin-orbit coupling schemes and conformational changes caused by excitation. The difference in the luminescent properties of 2,3-diphenyl-6-aminoquinoxalines from its examined analogs is due to a low energy of the S1(ππ*) level (21 200 cm-1 in alcohol), which is responsible for intense fluorescence (φf -0.5 in alcohol) and very weak phosphorescence.
- Rtishchev,Dobrodei,El'tsov
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p. 1658 - 1668
(2007/10/03)
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- Gould-Jacobs Reaction of 6-Amino-2,3-diphenylquinoxaline
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Catalytic hydrogenation of 2,3-diphenyl-6-nitroquinoxaline led to the corresponding amine 1 which in turn afforded products 3a-i on reaction with alkoxymethylene derivatives 2a-i.Thermal cyclization of 3b and 3f yielded substituted pyrazinoquinolones 5b a
- Milata, V.,Ilavsky, D.,Chudik, M.,Zalibera, L.,Lesko, J.,et al.
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p. 1349 - 1358
(2007/10/03)
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