Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization

Rare oncogenic NTRK gene fusions result in uncontrolled TRK signaling leading to various adult and pediatric solid tumors. Based on the architecture of our multi-targeted clinical candidate BPR1K871 (10), we designed and synthesized a series of quinazoline compounds as selective and orally bioavaila...

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Veröffentlicht in:	European journal of medicinal chemistry 2021-11, Vol.224, p.113673-113673, Article 113673
Hauptverfasser:	Li, Mu-Chun, Lin, Wen-Hsing, Wang, Pei-Chen, Su, Yu-Chieh, Chen, Pei-Yi, Fan, Chu-Min, Chen, Ching-Ping, Huang, Chen-Lung, Chiu, Chun-Hsien, Chang, Ling, Chen, Chiung-Tong, Yeh, Teng-Kuang, Hsieh, Hsing-Pang
Format:	Artikel
Sprache:	eng
Schlagworte:	Fusion Kinase inhibitor Mutation Property-driven optimization Tropomyosin receptor kinase (TRK)
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