1633819-04-1Relevant articles and documents
Discovery of novel 7-azaindole derivatives bearing dihydropyridazine moiety as c-Met kinase inhibitors
Tang, Qidong,Wang, Linxiao,Duan, Yongli,Wang, Wenhui,Huang, Shunmin,Zhi, Jia,Jia, Shuang,Zhu, Wufu,Wang, Ping,Luo, Rong,Zheng, Pengwu
, p. 97 - 106 (2017/04/07)
A series of 7-azaindole derivatives bearing the dihydropyridazine scaffold were synthesized and evaluated for their c-Met kinase inhibitory, and antiproliferative activity against 4 cancer cell lines (HT29, A549, H460, U87MG) were evaluated in?vitro. Most compounds showed moderate to excellent potency. Compared to foretinib, the most promising analog 34 (c-Met IC50: 1.06?nM, a multitarget tyrosine kinase inhibitor) showed a 6.4-, 7.8-, and 3.2-fold increase in activity against HT29, A549, and H460?cell lines, respectively. Structure activity relationship studies indicated that mono-EWGs (such as R2?=?F) at 4-position of moiety D was a key factor in improving the antitumor activity.