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10.1021/jm500660f http://scihub22266oqcxt.onion/10.1021/jm500660f C4207540!4207540 !25271760     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=25271760 &cmd=llinks): Failed to open stream: HTTP request failed! 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Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity |pdf=|usr=}}{{25271760 }} gab.com Text Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity JO: J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=25271760 #FOAvip Mutations of isocitrate dehydrogenase 1 (IDH1) are frequently found in certain cancers such as glioma. Different from the wild-type (WT) IDH1, the mutant enzymes catalyze the reduction of ?-ketoglutaric acid to d-2-hydroxyglutaric acid (D2HG), leading to cancer initiation. Several 1-hydroxypyridin-2-one compounds were identified to be inhibitors of IDH1(R132H). A total of 61 derivatives were synthesized, and their structure-activity relationships were investigated. Potent IDH1(R132H) inhibitors were identified with Ki values as low as 140 nM, while they possess weak or no activity against WT IDH1. Activities of selected compounds against IDH1(R132C) were found to be correlated with their inhibitory activities against IDH1(R132H), as well as cellular production of D2HG, with R(2) of 0.83 and 0.73, respectively. Several inhibitors were found to be permeable through the blood-brain barrier in a cell-based model assay and exhibit potent and selective activity (EC50 = 0.26-1.8 ?M) against glioma cells with the IDH1 R132H mutation. Twit Text FOAVip Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity ????J Med Chem http://www.kidney.de/pget.php?&tw=1&pmid=25271760 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=25271760 #FOAvip English Wikipedia <ref>{{Cite pmid|25271760 }}</ref> Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity #MMPMID25271760 Liu Z ; Yao Y ; Kogiso M ; Zheng B ; Deng L ; Qiu JJ ; Dong S ; Lv H ; Gallo JM ; Li XN ; Song Y J Med Chem 2014[Oct]; 57 (20 ): 8307-18 PMID25271760 show ga Mutations of isocitrate dehydrogenase 1 (IDH1) are frequently found in certain cancers such as glioma. Different from the wild-type (WT) IDH1, the mutant enzymes catalyze the reduction of ?-ketoglutaric acid to d-2-hydroxyglutaric acid (D2HG), leading to cancer initiation. Several 1-hydroxypyridin-2-one compounds were identified to be inhibitors of IDH1(R132H). A total of 61 derivatives were synthesized, and their structure-activity relationships were investigated. Potent IDH1(R132H) inhibitors were identified with Ki values as low as 140 nM, while they possess weak or no activity against WT IDH1. Activities of selected compounds against IDH1(R132C) were found to be correlated with their inhibitory activities against IDH1(R132H), as well as cellular production of D2HG, with R(2) of 0.83 and 0.73, respectively. Several inhibitors were found to be permeable through the blood-brain barrier in a cell-based model assay and exhibit potent and selective activity (EC50 = 0.26-1.8 ?M) against glioma cells with the IDH1 R132H mutation. |Animals [MESH] |Antineoplastic Agents/chemical synthesis/*chemistry/*pharmacology [MESH] |Blood-Brain Barrier/drug effects [MESH] |Brain Neoplasms/drug therapy/pathology [MESH] |Crystallography, X-Ray [MESH] |Drug Screening Assays, Antitumor [MESH] |Enzyme Inhibitors/chemical synthesis/chemistry/*pharmacology [MESH] |Glioma/drug therapy/pathology [MESH] |Glutarates/metabolism [MESH] |Humans [MESH] |Isocitrate Dehydrogenase/*antagonists & inhibitors/*genetics [MESH] |Mice [MESH] |Pyridones/chemistry [MESH] |Structure-Activity Relationship [MESH]Inhibition of cancer-associated mutant isocitrate dehydrogenases: synt(epmc).pdf DeepDyve Pubget Overpricing