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Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2–p53 and MDMX–p53 protein–protein interactions
2013
MedChemComm
Screening identified 2-(3-((4,6-dioxo-2-thioxotetrahydropyrimidin-5(2H)-ylidene)methyl)-2,5-dimethyl-1Hpyrrol-1-yl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile as an MDM2-p53 inhibitor (IC 50 ¼ 12.3 mM). MDM2-p53 and MDMX-p53 activity was seen for 5-((1-(4-chlorophenyl)-2,5-diphenyl-1H-pyrrol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione (MDM2 IC 50 ¼ 0.11 mM; MDMX IC 50 ¼ 4.2 mM) and
doi:10.1039/c3md00161j
pmid:24078862
pmcid:PMC3777193
fatcat:yg43jtpwp5hgtmb4guay4iij2u