Add to ORKGFrom a set of weakly potent lead compounds, using in silico screening and small library synthesis, a series of 2-alkyl-3-aryl-3-alkoxyisoindolinones has been identified as inhibitors of the MDM2-p53 interaction. Two of the most potent compounds, 2-benzyl-3-(4-chlorophenyl)-3-(3-hydroxypropoxy)-2,3-dihydroisoindol-1-one (76; IC(50) = 15.9 +/- 0.8 microM) and 3-(4-chlorophenyl)-3-(4-hydroxy-3,5-dimethoxybenzyloxy)-2-propyl-2,3-dihydroisoindol-1-one (79; IC(50) = 5.3 +/- 0.9 microM), induced p53-dependent gene transcription, in a dose-dependent manner, in the MDM2 amplified, SJSA human sarcoma cell line
The p53 pathway is disrupted in virtually every human tumor. In similar to 50% of human cancers, the...
To search for novel p53 activators, four series of novel (S)- and (R)-tryptophanol-derived oxazolois...
In Chapter 2, bis- and tris- arylsulfonamides, were investigated as possible inhibitors of the p53-M...
A series of 2-N-alkyl-3-aryl-3-alkoxyisoindolinones has been synthesised and evaluated as inhibitors...
Inhibition of the MDM2-p53 interaction has been shown to produce an antitumor effect, especially in ...
The design, synthesis and evaluation of 24 isoindolinones as potential inhibitors of the MDM2-p53 in...
The tumor suppressor protein p53, also known as the guardian of genoma, is a transcription factor th...
Blocking the interaction between the p53 tumor suppressor and its regulatory protein MDM2 is a promi...
Disruption of the MDM2-p53 protein-protein interaction with small molecules has been shown to reacti...
AbstractA novel class of small-molecule inhibitors of MDM2–p53 interaction with a (E)-3-benzylidenei...
A series of novel amino acid ester derivatives of 2,3-substituted isoindolinones was synthesized and...
The tumor suppressor protein p53, also know as the guardian of genoma, is a a transcription factor t...
The easily available 3-(hetero)arylidene-oxindoles are a privileged scaffold for compounds endowed w...
Indole-based modulators of p53-MDM2 interaction as antitumoral agents. The tumor suppressor protein ...
Inactivation of the function of tumor suppressor p53 is common in human cancers. In approximately ha...
The p53 pathway is disrupted in virtually every human tumor. In similar to 50% of human cancers, the...
To search for novel p53 activators, four series of novel (S)- and (R)-tryptophanol-derived oxazolois...
In Chapter 2, bis- and tris- arylsulfonamides, were investigated as possible inhibitors of the p53-M...
A series of 2-N-alkyl-3-aryl-3-alkoxyisoindolinones has been synthesised and evaluated as inhibitors...
Inhibition of the MDM2-p53 interaction has been shown to produce an antitumor effect, especially in ...
The design, synthesis and evaluation of 24 isoindolinones as potential inhibitors of the MDM2-p53 in...
The tumor suppressor protein p53, also known as the guardian of genoma, is a transcription factor th...
Blocking the interaction between the p53 tumor suppressor and its regulatory protein MDM2 is a promi...
Disruption of the MDM2-p53 protein-protein interaction with small molecules has been shown to reacti...
AbstractA novel class of small-molecule inhibitors of MDM2–p53 interaction with a (E)-3-benzylidenei...
A series of novel amino acid ester derivatives of 2,3-substituted isoindolinones was synthesized and...
The tumor suppressor protein p53, also know as the guardian of genoma, is a a transcription factor t...
The easily available 3-(hetero)arylidene-oxindoles are a privileged scaffold for compounds endowed w...
Indole-based modulators of p53-MDM2 interaction as antitumoral agents. The tumor suppressor protein ...
Inactivation of the function of tumor suppressor p53 is common in human cancers. In approximately ha...
The p53 pathway is disrupted in virtually every human tumor. In similar to 50% of human cancers, the...
To search for novel p53 activators, four series of novel (S)- and (R)-tryptophanol-derived oxazolois...
In Chapter 2, bis- and tris- arylsulfonamides, were investigated as possible inhibitors of the p53-M...