nsc228155 and benzofurazan

nsc228155 has been researched along with benzofurazan* in 1 studies

Other Studies

1 other study(ies) available for nsc228155 and benzofurazan

Article	Year
Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription. Bioorganic & medicinal chemistry letters, 2013, Oct-01, Volume: 23, Issue:19 Cyclic-AMP response-element binding protein (CREB) is a stimulus-activated transcription factor. Its transcription activity requires its binding with CREB-binding protein (CBP) after CREB is phosphorylated at Ser133. The domains involved for CREB-CBP interaction are kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP. Recent studies suggest that CREB is an attractive target for novel cancer therapeutics. To identify novel chemotypes as inhibitors of KIX-KID interaction, we screened the NCI-diversity set of compounds using a split renilla luciferase assay and identified 2-[(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide (compound 1, NSC228155) as a potent inhibitor of KIX-KID interaction. However, compound 1 was not particularly selective against CREB-mediated gene transcription in living HEK 293T cells. Further structure-activityrelationship studies identified 4-aniline substituted nitrobenzofurazans with improved selectivity. Topics: Antineoplastic Agents; Benzoxazoles; Cells, Cultured; CREB-Binding Protein; Cyclic N-Oxides; Gene Expression Regulation; HEK293 Cells; Humans; Inhibitory Concentration 50; Molecular Structure; Oxadiazoles; Protein Structure, Secondary; Structure-Activity Relationship	2013

Article

Year

Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription.

Bioorganic & medicinal chemistry letters, 2013, Oct-01, Volume: 23, Issue:19

Cyclic-AMP response-element binding protein (CREB) is a stimulus-activated transcription factor. Its transcription activity requires its binding with CREB-binding protein (CBP) after CREB is phosphorylated at Ser133. The domains involved for CREB-CBP interaction are kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP. Recent studies suggest that CREB is an attractive target for novel cancer therapeutics. To identify novel chemotypes as inhibitors of KIX-KID interaction, we screened the NCI-diversity set of compounds using a split renilla luciferase assay and identified 2-[(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio]pyridine 1-oxide (compound 1, NSC228155) as a potent inhibitor of KIX-KID interaction. However, compound 1 was not particularly selective against CREB-mediated gene transcription in living HEK 293T cells. Further structure-activityrelationship studies identified 4-aniline substituted nitrobenzofurazans with improved selectivity.

Topics: Antineoplastic Agents; Benzoxazoles; Cells, Cultured; CREB-Binding Protein; Cyclic N-Oxides; Gene Expression Regulation; HEK293 Cells; Humans; Inhibitory Concentration 50; Molecular Structure; Oxadiazoles; Protein Structure, Secondary; Structure-Activity Relationship

2013