The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria. It is an orally available hydrophobic inhibitor prodrug used as chemotherapeutic agents for the treatment of refractory acute myeloid leukemia. It is hydrolyzed by CES1
Type : Drug
Chemical_Nomenclature : cyclopentyl (2S)-2-[[(2R)-2-[(1S)-2-(hydroxyamino)-1-methoxy-2-oxoethyl]-4-methylpentanoyl]amino]-2-phenylacetate
Canonical SMILES : CC(C)CC(C(C(=O)NO)OC)C(=O)NC(C1=CC=CC=C1)C(=O)OC2CCCC2
InChI : InChI=1S\/C22H32N2O6\/c1-14(2)13-17(19(29-3)21(26)24-28)20(25)23-18(15-9-5-4-6-10-15)22(27)30-16-11-7-8-12-16\/h4-6,9-10,14,16-19,28H,7-8,11-13H2,1-3H3,(H,23,25)(H,24,26)\/t17-,18+,19+\/m1\/s1
InChIKey : NYGGUGZLUBNLTJ-QYZOEREBSA-N
Other name(s) : CHR 2863 || CHR2863 || Cyclopentyl (2S)-2-[[(2R)-2-[(1S)-2-(hydroxyamino)-1-methoxy-2-oxo-ethyl]-4-methyl-pentanoyl]amino]-2-phenyl-acetate
MW : 420.49
Formula : C22H32N2O6
CAS_number :
PubChem : 15547707
UniChem : NYGGUGZLUBNLTJ-QYZOEREBSA-N
Structures : No structure
Families : Carb_B_Chordata
Title : Multifactorial resistance to aminopeptidase inhibitor prodrug CHR2863 in myeloid leukemia cells: down-regulation of carboxylesterase 1, drug sequestration in lipid droplets and pro-survival activation ERK\/Akt\/mTOR - Verbrugge_2016_Oncotarget_7_5240 |
Author(s) : Verbrugge SE , Al M , Assaraf YG , Kammerer S , Chandrupatla DM , Honeywell R , Musters RP , Giovannetti E , O'Toole T , Scheffer GL , Krige D , de Gruijl TD , Niessen HW , Lems WF , Kramer PA , Scheper RJ , Cloos J , Ossenkoppele GJ , Peters GJ , Jansen G |
Ref : Oncotarget , 7 :5240 , 2016 |
Abstract : |
PubMedSearch : Verbrugge_2016_Oncotarget_7_5240 |
PubMedID: 26496029 |
Title : The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria - Skinner-Adams_2012_Antimicrob.Agents.Chemother_56_3244 |
Author(s) : Skinner-Adams TS , Peatey CL , Anderson K , Trenholme KR , Krige D , Brown CL , Stack C , Nsangou DM , Mathews RT , Thivierge K , Dalton JP , Gardiner DL |
Ref : Antimicrobial Agents & Chemotherapy , 56 :3244 , 2012 |
Abstract : |
PubMedSearch : Skinner-Adams_2012_Antimicrob.Agents.Chemother_56_3244 |
PubMedID: 22450967 |