Discovery and Optimization of 2
Animals
Brain
/ metabolism
Cell Line, Tumor
Drug Evaluation, Preclinical
Enzyme Inhibitors
/ chemistry
Female
Glycine
/ analogs & derivatives
Half-Life
Humans
Isocitrate Dehydrogenase
/ antagonists & inhibitors
Mice
Mice, Nude
Microsomes, Liver
/ metabolism
Mutagenesis, Site-Directed
Neoplasms
/ drug therapy
Pyridines
/ therapeutic use
Pyridones
/ chemistry
Rats
Structure-Activity Relationship
Xenograft Model Antitumor Assays
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
22 04 2021
22 04 2021
Historique:
pubmed:
7
4
2021
medline:
16
6
2021
entrez:
6
4
2021
Statut:
ppublish
Résumé
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia. We report a medicinal chemistry campaign around a 7,7-dimethyl-7,8-dihydro-2
Identifiants
pubmed: 33822623
doi: 10.1021/acs.jmedchem.1c00019
pmc: PMC8968748
mid: NIHMS1769820
doi:
Substances chimiques
Enzyme Inhibitors
0
Pyridines
0
Pyridones
0
Isocitrate Dehydrogenase
EC 1.1.1.41
IDH1 protein, human
EC 1.1.1.42.
ivosidenib
Q2PCN8MAM6
Glycine
TE7660XO1C
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, N.I.H., Intramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
4913-4946Subventions
Organisme : CCR NIH HHS
ID : HHSN261200800001C
Pays : United States
Organisme : NCI NIH HHS
ID : HHSN261200800001E
Pays : United States
Organisme : Intramural NIH HHS
ID : Z99 TR999999
Pays : United States
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