17796-60-0Relevant academic research and scientific papers
Design, synthesis, biological evaluation and molecular docking study on peptidomimetic analogues of XK469
Xia, Qiao-Hong,Hu, Wei,Li, Chen,Wu, Ji-Feng,Yang, Liang,Han, Xue-Mei,Shen, Yue-Mao,Li, Zhi-Yu,Li, Xun
supporting information, p. 311 - 325 (2016/09/07)
XK469 is identified as a potent quinoxaline antineoplastic agent based on its significant clinical efficacy. It probably exerts its activity via DNA topoisomerase II (topo II) inhibition. To obtain more effective antineoplastic agents, a spectrum of peptidomimetic-type quinoxaline analogues of XK469 was herein designed, synthesized, and evaluated. Few compounds (e.g. 13a and 13b) exhibited obvious cytotoxicity indicated by in?vitro anti-proliferative assay. SAR investigation revealed that introducing of hydrophobic tert-butylamine or dodecylamine moiety at the 3-position of quinoxaline core is favorable for achieving a better anti-proliferative potency, while peptidomimetic derivatives only yielded moderate cytotoxicity. Compounds with improved anti-proliferative activities also demonstrated decent anti-metastatic potencies comparable with that of doxorubicin (Doxo) based on in?vivo mouse model study. The topo II-mediated kinetoplast DNA (kDNA) decatenation assay as well as molecular docking studies implicated that these compounds tend to be potent topo II inhibitors. Overall, compounds 13a and 13b, 13b in particular, standed out from various assessments and might be promising candidates for further chemical optimization.
Aqueous hydrofluoric acid catalyzed facile synthesis of 2,3,6-substituted quinoxalines
Chandra Shekhar,Ravi Kumar,Sathaiah,Raju,Srinivas,Shanthan Rao,Narsaiah
, p. 1504 - 1508 (2015/04/27)
A versatile synthetic route for the preparation of 2,3,6-trisubstituted quinoxalines in excellent yield is developed from θ-diamines and 1,2-dicarbonyl compounds in which aqueous hydrofluoric acid was employed as the medium and catalyst. Other salient features of this protocol include milder conditions, absence of coupling agents, and easy workup procedures.
TRIAZOLOPYRAZINE DERIVATIVES AND THEIR USE FOR TREATING NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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Page/Page column 19, (2013/03/26)
The present invention is directed to triazolopyrazine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.
TRIAZOLO COMPOUNDS AS PDE10 INHIBITORS
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Page/Page column 161, (2014/01/07)
The present invention provides compounds of formula (Ia) and (Ib) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
(1,2,4)TRIAZOLO[4,3-A]QUINOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASES
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Page/Page column 41, (2012/08/27)
The invention relates to (1,2,4)triazolo[4,3-a]quinoxaline derivatives of Formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases.
Synthesis of some new 2-(3-methyl-7-substituted-2-oxoquinoxalinyl)-5-(aryl) -1,3,4-oxadiazoles as potential non-steroidal anti-inflammatory and analgesic agents
Wagle, Shivananda,Adhikari, Airody Vasudeva,Kumari, Nalilu Suchetha
, p. 439 - 448 (2008/09/20)
Ethyl (3-methyl-7-substituted-2-oxoquinoxalin-1(2H)-yl) acetates 2a-c are prepared by the condensation of ethyl chloroacetate with 3-methyl-7-substituted quinoxalin-2(1H)-ones 1a-c. The reaction of 2a-c with hydrazine hydrate furnished 2-(3-methyl-7-substituted-2-oxoquinoxalin-1(2H)-yl) acetohydrazides 3a-c, which on cyclisation with substituted aromatic carboxylic acids in the presence of phosphorous oxychloride give 3-methyl-7-substituted-1-[(5-aryl-1,3, 4-oxadiazol-2-yl)methyl]quinoxalin-2(1H)-ones 4a-y. Further, the compounds 3a-c on cyclisation with carbon disulphide in methanolic potassium hydroxide yielded 1-[(5-mercapto-1,3,4-oxadiazol-2-yl)methyl]-3-methyl-7-substituted quinoxalin-2(1H)-ones 5a-c. Finally, the compounds 5a-c are converted to 3-methyl-7-substituted-1-{[5-(alkylsulfanyl)-1,3,4-oxadiazol-2-yl]methyl} quinoxalin-2(1H)-ones 6a-i by reacting them with different alkyl halides. The newly synthesized compounds have been characterized by IR, 1H NMR, 13C NMR and mass spectral data and elemental analysis. Selected compounds are screened for in vivo anti-inflammatory and analgesic activity. Few of them exhibited promising activity.
NON-PEPTIDE GLP-1 AGONISTS
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Page/Page column 48-49, (2010/02/13)
Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an ac
