{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Penthala NR"],"funding":["NCI","Arkansas Research Alliance","NCI NIH HHS","NIH"],"pagination":["7226-33"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4747820"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["23(22)"],"pubmed_abstract":["In the present study, we have designed and synthesized a series of 1-benzyl-2-methyl-3-indolylmethylene barbituric acid analogs (7a-7h) and 1-benzyl-2-methyl-3-indolylmethylene thiobarbituric acid analogs (7 i-7 l) as nucleophosmin 1 (NPM1) inhibitors and have evaluated them for their anti-cancer activity against a panel of 60 different human cancer cell lines. Among these analogs 7 i, 7 j, and 7 k demonstrated potent growth inhibitory effects in various cancer cell types with GI50 values <2 μM. Compound 7 k exhibited growth inhibitory effects on a sub-panel of six leukemia cell lines with GI50 values in the range 0.22-0.35 μM. Analog 7 i also exhibited GI50 values <0.35 μM against three of the leukemia cell lines in the sub-panel. Analogs 7 i, 7 j, 7 k and 7 l were also evaluated against "],"journal":["Bioorganic & medicinal chemistry"],"pubmed_title":["1-Benzyl-2-methyl-3-indolylmethylene barbituric acid derivatives: Anti-cancer agents that target nucleophosmin 1 (NPM1)."],"pmcid":["PMC4747820"],"funding_grant_id":["R01 CA183895","R01 CA140409","CA 183895","CA 140409"],"pubmed_authors":["Balusu R","Ketkar A","Sekhar KR","Eoff RL","Penthala NR","Freeman ML","Crooks PA"],"additional_accession":[]},"is_claimable":false,"name":"1-Benzyl-2-methyl-3-indolylmethylene barbituric acid derivatives: Anti-cancer agents that target nucleophosmin 1 (NPM1).","description":"In the present study, we have designed and synthesized a series of 1-benzyl-2-methyl-3-indolylmethylene barbituric acid analogs (7a-7h) and 1-benzyl-2-methyl-3-indolylmethylene thiobarbituric acid analogs (7 i-7 l) as nucleophosmin 1 (NPM1) inhibitors and have evaluated them for their anti-cancer activity against a panel of 60 different human cancer cell lines. Among these analogs 7 i, 7 j, and 7 k demonstrated potent growth inhibitory effects in various cancer cell types with GI50 values <2 μM. Compound 7 k exhibited growth inhibitory effects on a sub-panel of six leukemia cell lines with GI50 values in the range 0.22-0.35 μM. Analog 7 i also exhibited GI50 values <0.35 μM against three of the leukemia cell lines in the sub-panel. Analogs 7 i, 7 j, 7 k and 7 l were also evaluated against ","dates":{"release":"2015-01-01T00:00:00Z","publication":"2015 Nov","modification":"2026-05-04T08:12:40.265Z","creation":"2019-03-27T02:08:48Z"},"accession":"S-EPMC4747820","cross_references":{"pubmed":["26602084"],"doi":["10.1016/j.bmc.2015.10.019"]}}