@article{97496161f83a4de9b265438b984a863e,
title = "2-Amino-2,3-dihydro-1 H-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy",
abstract = "A series of 2-amino-2,3-dihydro-1H-indene-5-carboxamides were designed and synthesized as new selective discoidin domain receptor 1 (DDR1) inhibitors. One of the representative compounds, 7f, bound with DDR1 with a Kd value of 5.9 nM and suppressed the kinase activity with an half-maximal (50%) inhibitory concentration value of 14.9 nM. 7f potently inhibited collagen-induced DDR1 signaling and epithelial-mesenchymal transition, dose-dependently suppressed colony formation of pancreatic cancer cells, and exhibited promising in vivo therapeutic efficacy in orthotopic mouse models of pancreatic cancer.",
author = "Dongsheng Zhu and Huocong Huang and Pinkas, {Daniel M.} and Jinfeng Luo and Debolina Ganguly and Fox, {Alice E.} and Emily Arner and Qiuping Xiang and Tu, {Zheng Chao} and Bullock, {Alex N.} and Brekken, {Rolf A.} and Ke Ding and Xiaoyun Lu",
note = "Funding Information: The authors appreciate the financial support from National Natural Science Foundation of China (81820108029, 21572230, 81673285, and 81425021), Guangdong Province (2015A030312014, 2015A030306042, and 2016A050502041), Guangzhou city (201805010007), and Jinan University. We also thank Diamond Light Source for beamtime (proposal mx15433), as well as the staff of beamline I04 for assistance with data collection. The SGC is a registered charity (number 1097737) that receives funds from AbbVie, Bayer Pharma AG, Boehringer Ingelheim, Canada Foundation for Innovation, Eshelman Institute for Innovation, Genome Canada, Innovative Medicines Initiative (EU/EFPIA) (ULTRA-DD grant no. 115766), Janssen, Merck KGaA Darmstadt Germany, MSD, Novartis Pharma AG, Ontario Ministry of Economic Development and Innovation, Pfizer, S{\~a}o Paulo Research Foundation-FAPESP, Takeda, and Wellcome (106169/ZZ14/Z). Publisher Copyright: Copyright {\textcopyright} 2019 American Chemical Society.",
year = "2019",
month = aug,
day = "22",
doi = "10.1021/acs.jmedchem.9b00365",
language = "English (US)",
volume = "62",
pages = "7431--7444",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "16",
}