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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.

Original publication

DOI

10.1021/acs.jmedchem.9b00365

Type

Journal article

Journal

J Med Chem

Publication Date

22/08/2019

Volume

62

Pages

7431 - 7444

Keywords

Animals, Antineoplastic Agents, Cell Line, Tumor, Discoidin Domain Receptor 1, Drug Design, Epithelial-Mesenchymal Transition, Humans, Male, Mice, Inbred C57BL, Neoplasms, Experimental, Pancreatic Neoplasms, Rats, Sprague-Dawley, Tumor Stem Cell Assay, Xenograft Model Antitumor Assays