208519-10-2Relevant articles and documents
Discovery of mixed type thymidine phosphorylase inhibitors endowed with antiangiogenic properties: Synthesis, pharmacological evaluation and molecular docking study of 2-thioxo-pyrazolo[1,5-a][1,3,5]triazin-4-ones. Part II
Bera, Hriday,Ojha, Probir Kumar,Tan, Bee Jen,Sun, Lingyi,Dolzhenko, Anton V.,Chui, Wai-Keung,Chiu, Gigi Ngar Chee
, p. 294 - 303 (2014/04/17)
In our drug discovery program, a series of 2-thioxo-pyrazolo[1,5-a][1,3,5] triazin-4-ones were designed, synthesized and evaluated for their TP inhibitory potential. All the synthesized analogues conferred a varying degree of TP inhibitory activity, comparable or better than positive control, 7-deazaxanthine (7-DX, 2) (IC50 value = 42.63 μM). A systematic approach to the lead optimization identified compounds 3c and 4a as the most promising TP inhibitors, exhibiting mixed mode of enzyme inhibition. Moreover, selected compounds demonstrated the ability to attenuate the expression of the angiogenic markers (viz. MMP-9 and VEGF) in MDA-MB-231 cells at sublethal concentrations. In addition, molecular docking studies revealed the plausible binding orientation of these inhibitors towards TP, which was in accordance with the experimental results. Taken as a whole, these compounds would constitute a new direction for the design of novel TP inhibitors with promising antiangiogenic properties.
Methods of treating conditions associated with an EDG-4 receptor
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, (2008/06/13)
The present invention provides a method of modulating an Edg-4 receptor mediated biological activity in a cell. A cell expressing the Edg-4 receptor is contacted with a modulator of an Edg-4 receptor sufficient to modulate the Edg-4 receptor mediated biol
Aminopyrazole derivatives
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, (2008/06/13)
PCT No. PCT/JP97/04571 Sec. 371 Date Jul. 30, 1999 Sec. 102(e) Date Jul. 30, 1999 PCT Filed Dec. 12, 1997 PCT Pub. No. WO98/25908 PCT Pub. Date Jun. 18, 1998The present invention relates to a compound represented by the general formula [I]: wherein Ar1 re
Urea derivatives
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, (2008/06/13)
The present invention relates to a compound represented by the general formula [I]: STR1 wherein A represents a nitrogen atom or a group represented by C--R5 ; Ar1 represents an aryl group which may have a substituent selected from t
Pyrazole derivatives
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, (2008/06/13)
The present invention relates to a compound represented by the general formula [I]: wherein A and B rings are ortho-condensed to each other, A ring represents an aromatic carbocyclic or heterocyclic ring and B ring represents an aliphatic four- to seven-m