Discovery of EBI-907: A highly potent and orally active B-RafV600Einhibitor for the treatment of melanoma and associated cancers

DOI: 10.1016/j.bmcl.2015.12.086

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 819 - 823 (2016)

Update date:2022-08-02

Topics: Discovery Potent Orally Active Experimental Melanoma

Authors:

Lu, Biao

Cao, Hu Cao, Hu

Cao, Jingsong

Huang, Song

Hu, Qiyue

Liu, Dong

Shen, Ru

Shen, Xiaodong

Tao, Weikang

Wan, Hong

Wang, Dan

Yan, Yinfa

Yang, Liuqing

Zhang, Jiayin

Zhang, Lei

Zhang, Lianshan

Zhang, Minsheng

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Article abstract of DOI:10.1016/j.bmcl.2015.12.086

A novel series of pyrazolo[3,4-c]isoquinoline derivatives was discovered as B-Raf^V600Einhibitors through scaffold hopping based on a literature lead PLX4720. Further SAR exploration and optimization led to the discovery of potent B-Raf^V600

Full text of DOI:10.1016/j.bmcl.2015.12.086

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