{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Morgen M"],"funding":["NCRR NIH HHS","Argonne National Laboratory","National Institutes of Health","NIGMS NIH HHS"],"pagination":["1163-1174"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC7335359"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["15(13)"],"pubmed_abstract":["We report the synthesis and evaluation of a class of selective multitarget agents for the inhibition of HDAC6, HDAC8, and HDAC10. The concept for this study grew out of a structural analysis of the two selective inhibitors Tubastatin A (HDAC6/10) and PCI-34051 (HDAC8), which we recognized share the same N-benzylindole core. Hybridization of the two inhibitor structures resulted in dihydroxamic acids with benzyl-indole and -indazole core motifs. These substances exhibit potent activity against HDAC6, HDAC8, and HDAC10, while retaining selectivity over HDAC1, HDAC2, and HDAC3. The best substance inhibited the viability of the SK-N-BE(2)C neuroblastoma cell line with an IC<sub>50</sub> value similar to a combination treatment with Tubastatin A and PCI-34051. This compound class establishes a "],"journal":["ChemMedChem"],"pubmed_title":["Design and Synthesis of Dihydroxamic Acids as HDAC6/8/10 Inhibitors."],"pmcid":["PMC7335359"],"funding_grant_id":["R01 GM049758","DE-AC02-06CH11357","P30 GM124165","GM49758","S10 RR029205","T32 GM071339"],"pubmed_authors":["Oehme I","Miller AK","Herbst-Gervasoni CJ","Steimbach RR","Christianson DW","Ridinger J","Sehr P","Porter NJ","Witt O","Osko JD","Gunkel N","Hellweg L","Morgen M","Geraldy M"],"additional_accession":[]},"is_claimable":false,"name":"Design and Synthesis of Dihydroxamic Acids as HDAC6/8/10 Inhibitors.","description":"We report the synthesis and evaluation of a class of selective multitarget agents for the inhibition of HDAC6, HDAC8, and HDAC10. The concept for this study grew out of a structural analysis of the two selective inhibitors Tubastatin A (HDAC6/10) and PCI-34051 (HDAC8), which we recognized share the same N-benzylindole core. Hybridization of the two inhibitor structures resulted in dihydroxamic acids with benzyl-indole and -indazole core motifs. These substances exhibit potent activity against HDAC6, HDAC8, and HDAC10, while retaining selectivity over HDAC1, HDAC2, and HDAC3. The best substance inhibited the viability of the SK-N-BE(2)C neuroblastoma cell line with an IC<sub>50</sub> value similar to a combination treatment with Tubastatin A and PCI-34051. This compound class establishes a ","dates":{"release":"2020-01-01T00:00:00Z","publication":"2020 Jul","modification":"2026-04-30T05:55:01.253Z","creation":"2020-07-09T07:01:43Z"},"accession":"S-EPMC7335359","cross_references":{"pubmed":["32348628"],"doi":["10.1002/cmdc.202000149"]}}