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

• Автори: Ashraf K. El-Damasy (Автор), Hyun Ji Kim (Автор), Jung Woo Park (Автор), Yunju Nam (Автор), Wooyoung Hur (Автор), Eun-Kyoung Bang (Автор), Gyochang Keum (Автор)
• Формат: Книга
• Опубліковано: Taylor & Francis Group, 2023-12-01T00:00:00Z.
• Предмети: article
• Онлайн доступ: Connect to this object online.

BCR-ABL inhibition is an effective therapeutic approach for the treatment of chronic myeloid leukaemia (CML). Herein, we report the discovery of AKE-72 (5), a diarylamide 3-aminoindazole, as a potent pan-BCR-ABL inhibitor, including the imatinib-resistant mutant T315I. A focussed array of compounds...