Journal of Medicinal Chemistry p. 8200 - 8215 (2015)
Update date:2022-09-26
Topics:
Zeng, Qingbei
Wang, Jiabing
Cheng, Ziqiang
Chen, Kan
Johnstr?m, Peter
Varn?s, Katarina
Li, David Yunzhi
Yang, Zhen Fan
Zhang, Xiaolin
Recent reports suggest that an increasing number of patients with lung cancer, especially those with activating mutations of the epidermal growth factor receptor (EGFR), also present with brain metastases and leptomeningeal metastases. These patients have poor prognosis as there are no approved drugs for these indications. Available agents have poor efficacy for these patients even at well above their standard dose. Herein, we report the discovery of (4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carboxylate 1m (AZD3759), an investigational drug currently in Phase 1 clinical trial, which has excellent central nervous system penetration and which induces profound regression of brain metastases in a mouse model.
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