Design, synthesis and biological evaluation of novel 1H-1,2,4-triazole, benzothiazole and indazole-based derivatives as potent FGFR1 inhibitors viafragment-based virtual screening

• Main Authors: Jian Liu (Author), Yu Wen (Author), Lina Gao (Author), Liang Gao (Author), Fengjun He (Author), Jingxian Zhou (Author), Junwei Wang (Author), Rupeng Dai (Author), Xiaojing Chen (Author), Di Kang (Author), Lihong Hu (Author)
• Format: Book
• Published: Taylor & Francis Group, 2020-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Fibroblast growth-factor receptor (FGFR) is a potential target for cancer therapy. We designed three novel series of FGFR1 inhibitors bearing indazole, benzothiazole, and 1H-1,2,4-triazole scaffold via fragment-based virtual screening. All the newly synthesised compounds were evaluated in vitro for...