3775-05-1Relevant academic research and scientific papers
NOVEL PYRIDOPYRIMIDINONE COMPOUNDS FOR MODULATING THE CATALYTIC ACTIVITY OF HISTONE LYSINE DEMETHYLASES (KDMS)
-
Page/Page column 98-99, (2016/05/19)
The present invention provides a compound of Formula (I) being capable of modulating the activity of histone lysine demethylase (KDM), pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament. The compound of Formula (I) acts as KDM inhibitor with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to KDM dysregulation.
Synthesis of salicylaldehydes from phenols via copper-mediated duff reaction
Fu, Xue-Wen,Pu, Wen-Chen,Zhang, Guo-Lin,Wang, Chun
, p. 8147 - 8158 (2015/02/19)
A copper-mediated Duff reaction for ortho-selective formylation of phenols has been developed. In the presence of copper species, significant improvements of yield and ortho-selectivity of the Duff formylation were achieved, which provides an easy access to salicylaldehydes from phenols.
Studies on benzofuran-7-carboxamides as poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors
Lee, Sunkyung,Yi, Kyu Yang,Lee, Byung Ho,Oh, Kwang Seok
, p. 1147 - 1153 (2012/07/14)
Benzofuran-7-carboxamide was identified as a novel scaffold of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. A series of compounds with various 2-substituents including (tertiary amino)methyl moieties substituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluated to elucidate the structure-activity relationships and optimize the potency. 2-[4-(Pyrrolidin-1-ylmethyl)phenyl]-benzofuran-7- carboxamide (42) was the most potent as an IC50 value of 40 nM among those.
Salicylic acid derivatives, processes for their preparation, compositions comprising them, their use
-
, (2008/06/13)
Salicylic acid derivatives of the formula I, where the index and the substituents have the following meanings: X is halogen, NO2, cyano, alkyl or alkoxy; m is 0, 1, 2 or 3, it being possible for the substituents X to be different from each othe
Benzo-furan derivative
-
, (2008/06/13)
Novel benzo-furan(or -thiophene) derivative of the formula: STR1 wherein R1 is hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl-lower alkyl group or a substituted or unsubstituted phenyl group, R2 is hydrogen atom, a lower alkyl group, an acyl group or phenyl group, R3 is hydrogen atom, a halogen atom, nitro group, a lower alkoxy group, amino group or an acylamino group, R4 is a group of the formula: STR2 A is a lower alkylene group optionally substituted with hydroxy group, B is single bond or a lower alkylene group, one of R5 and R6 is hydrogen atom or a lower alkyl group and the other is a lower alkyl group or a phenyl-lower alkyl group, or R5 and R6 combine together with adjacent nitrogen atom to form a heteromonocyclic group, R7 is a lower alkyl group, X is oxygen atom or sulfur atom, Y is oxygen atom, imino group, a lower alkylimino group or a phenyl-lower alkylimino group and a salt thereof are disclosed. Said compound (I) and a salt thereof have a potent inhibitory activity against reflective contraction of urinary bladder.
Benzofuran derivative and processes for preparing the same
-
, (2008/06/13)
A novel benzofuran derivative of the formula: STR1 wherein R1 is hydrogen atom, a lower alkoxy group or a halogen atom, one of R2 and R3 is a lower alkyl group and the other is a lower alkyl group or a phenyl-lower alkyl g
