Small‐molecule MDM2 inhibitor LQFM030‐induced apoptosis in p53‐null K562 chronic myeloid leukemia cells

Our group designed and synthesized the N‐phenyl‐piperazine LQFM030 [1‐(4‐((1‐(4‐chlorophenyl)‐1H–pyrazol‐4‐yl)methyl) piperazin‐1‐yl) ethanone], a small molecule derived from molecular simplification of the Nutlin‐1, an inhibitor of the human homologue of murine double minute 2 (MDM2) protein that i...

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Veröffentlicht in:	Fundamental & clinical pharmacology 2020-08, Vol.34 (4), p.444-457
Hauptverfasser:	Oliveira Ribeiro, Higor, Cortez, Alane Pereira, Ávila, Renato Ivan, Silva, Artur Christian Garcia, Carvalho, Flávio Silva, Menegatti, Ricardo, Lião, Luciano Morais, Valadares, Marize Campos
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - pharmacology Apoptosis Apoptosis - drug effects Apoptosis Regulatory Proteins - genetics Apoptosis Regulatory Proteins - metabolism BALB 3T3 Cells Cancer Caspase Cell activation Cell cycle Cell death Chronic myeloid leukemia Cytotoxicity Drug development drug discovery Enzyme Inhibitors - pharmacology Homology Humans Inhibitors K562 Cells Leukemia Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology Leukemia, Myelogenous, Chronic, BCR-ABL Positive - genetics Leukemia, Myelogenous, Chronic, BCR-ABL Positive - pathology MDM2 MDM2 protein Mice Mitochondria Mutation Myc protein Myeloid leukemia nutlins p53 p53 Protein Pharmacology Piperazine Piperidines - pharmacology Proto-Oncogene Proteins c-mdm2 - antagonists & inhibitors Proto-Oncogene Proteins c-mdm2 - metabolism Pyrazoles - pharmacology Signal Transduction Transcription Tumor Suppressor Protein p53 - deficiency Tumor Suppressor Protein p53 - genetics
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