A Kinase Inhibitor with Anti-Pim Kinase Activity is a Potent and Selective Cytotoxic Agent Toward Acute Myeloid Leukemia.
Apoptosis
/ drug effects
Carbazoles
/ chemistry
Cell Line, Tumor
Cell Proliferation
/ drug effects
Cytarabine
/ chemistry
Humans
Indazoles
/ chemistry
Leukemia, Myeloid, Acute
/ drug therapy
Mutation
/ drug effects
Phosphorylation
/ drug effects
Protein Kinase Inhibitors
/ chemistry
Proto-Oncogene Proteins c-pim-1
/ antagonists & inhibitors
Signal Transduction
/ drug effects
Topoisomerase II Inhibitors
/ chemistry
Journal
Molecular cancer therapeutics
ISSN: 1538-8514
Titre abrégé: Mol Cancer Ther
Pays: United States
ID NLM: 101132535
Informations de publication
Date de publication:
03 2019
03 2019
Historique:
received:
13
12
2017
revised:
05
05
2018
accepted:
14
01
2019
pubmed:
27
1
2019
medline:
13
3
2020
entrez:
26
1
2019
Statut:
ppublish
Résumé
More than 40 years ago, the present standard induction therapy for acute myeloid leukemia (AML) was developed. This consists of the metabolic inhibitor cytarabine (AraC) and the cytostatic topoisomerase 2 inhibitor daunorubucin (DNR). In light of the high chance for relapse, as well as the large heterogeneity, novel therapies are needed to improve patient outcome. We have tested the anti-AML activity of 15 novel compounds based on the scaffolds pyrrolo[2,3-
Identifiants
pubmed: 30679386
pii: 1535-7163.MCT-17-1234
doi: 10.1158/1535-7163.MCT-17-1234
doi:
Substances chimiques
Carbazoles
0
Indazoles
0
Protein Kinase Inhibitors
0
Topoisomerase II Inhibitors
0
Cytarabine
04079A1RDZ
carbazole
0P2197HHHN
Proto-Oncogene Proteins c-pim-1
EC 2.7.11.1
proto-oncogene proteins pim
EC 2.7.11.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
567-578Informations de copyright
©2019 American Association for Cancer Research.