Discovery of 3-((3-amino-<i>1H</i>-indazol-4-yl)ethynyl)-<i>N</i>-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide (AKE-72), a potent Pan-BCR-ABL inhibitor including the T315I gatekeeper resistant mutant.

El-Damasy, Ashraf K; Kim, Hyun Ji; Park, Jung Woo; Nam, Yunju; Hur, Wooyoung; Bang, Eun-Kyoung; Keum, Gyochang

Discovery of 3-((3-amino-1H-indazol-4-yl)ethynyl)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide (AKE-72), a potent Pan-BCR-ABL inhibitor including the T315I gatekeeper resistant mutant.

El-Damasy, Ashraf K; Kim, Hyun Ji; Park, Jung Woo; Nam, Yunju; Hur, Wooyoung; Bang, Eun-Kyoung; Keum, Gyochang.

Afiliação

El-Damasy AK; Brain Science Institute, Korea Institute of Science and Technology (KIST), Seoul, Republic of Korea.
Kim HJ; Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
Park JW; Brain Science Institute, Korea Institute of Science and Technology (KIST), Seoul, Republic of Korea.
Nam Y; Supercomputing Application Center, Div. of National Supercomputing, Korea Institute of Science and Technology Information, Daejeon, Republic of Korea.
Hur W; Medicinal Materials Research Center, Korea Institute of Science and Technology (KIST), Seoul, Republic of Korea.
Bang EK; Medicinal Materials Research Center, Korea Institute of Science and Technology (KIST), Seoul, Republic of Korea.
Keum G; Brain Science Institute, Korea Institute of Science and Technology (KIST), Seoul, Republic of Korea.

J Enzyme Inhib Med Chem ; 38(1): 2228515, 2023 Dec.

Article em En | MEDLINE | ID: mdl-37470410

Assuntos

Indazóis; Leucemia Mielogênica Crônica BCR-ABL Positiva; Humanos; Indazóis/farmacologia; Resistencia a Medicamentos Antineoplásicos; Mesilato de Imatinib/farmacologia; Mesilato de Imatinib/uso terapêutico; Inibidores de Proteínas Quinases/farmacologia; Inibidores de Proteínas Quinases/uso terapêutico; Proteínas de Fusão bcr-abl/genética; Proteínas de Fusão bcr-abl/metabolismo; Benzamidas/farmacologia; Linhagem Celular Tumoral; Leucemia Mielogênica Crônica BCR-ABL Positiva/tratamento farmacológico; Leucemia Mielogênica Crônica BCR-ABL Positiva/genética; Leucemia Mielogênica Crônica BCR-ABL Positiva/metabolismo; Mutação; Proliferação de Células; Apoptose

Palavras-chave

ABLT315I; Chronic myeloid leukaemia; Imatinib resistance; aminoindazole; diarylamides

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Leucemia Mielogênica Crônica BCR-ABL Positiva / Indazóis Limite: Humans Idioma: En Ano de publicação: 2023 Tipo de documento: Article

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