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Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-02-01 , DOI: 10.1016/j.bmcl.2019.01.037 Changwei Chen 1 , Peichen Pan 1 , Ziyang Deng 1 , Dahai Wang 1 , Qifan Wu 1 , Lei Xu 2 , Tingjun Hou 1 , Sunliang Cui 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2019-02-01 , DOI: 10.1016/j.bmcl.2019.01.037 Changwei Chen 1 , Peichen Pan 1 , Ziyang Deng 1 , Dahai Wang 1 , Qifan Wu 1 , Lei Xu 2 , Tingjun Hou 1 , Sunliang Cui 1
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A new series of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridine compounds have been discovered as potent anaplastic lymphoma kinase (ALK) inhibitors. The 4-hydroxyphenyl in the 6-position of 1H-pyrazolo[3,4-b]pyridine were crucial and a fluorine atom substitution could give promising inhibitory activity. The IC50 of compound 9v against ALK was up to 1.58 nM and a binding mechanism was proposed.
中文翻译：
发现3,6-二芳基-1H-吡唑并[3,4-b]吡啶类为有效的间变性淋巴瘤激酶（ALK）抑制剂。
已经发现了一系列新的3，6-二芳基-1H-吡唑并[3，4-b]吡啶化合物作为有效的间变性淋巴瘤激酶（ALK）抑制剂。1H-吡唑并[3,4-b]吡啶的6-位上的4-羟基苯基至关重要，氟原子取代可以提供有希望的抑制活性。化合物9v对ALK的IC50高达1.58 nM，并提出了一种结合机制。
更新日期：2019-02-01
中文翻译：
发现3,6-二芳基-1H-吡唑并[3,4-b]吡啶类为有效的间变性淋巴瘤激酶（ALK）抑制剂。
已经发现了一系列新的3，6-二芳基-1H-吡唑并[3，4-b]吡啶化合物作为有效的间变性淋巴瘤激酶（ALK）抑制剂。1H-吡唑并[3,4-b]吡啶的6-位上的4-羟基苯基至关重要，氟原子取代可以提供有希望的抑制活性。化合物9v对ALK的IC50高达1.58 nM，并提出了一种结合机制。
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