Journal article

2-amino-2, 3-dihydro-1H-indene-5-carboxamide-based discoidin domain receptors 1 (DDR1) inhibitors: design, synthesis, and in vivo anti-pancreatic 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.

Publication status:: Published

Peer review status:: Peer reviewed

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APA Style

Zhu, D., Huang, H., Pinkas, D., Luo, J., Ganguly, D., Fox, A., Arner, E., Xiang, Q., Tu, Z., Bullock, A., Brekken, R., Ding, K., & Lu, X. (2019). 2-amino-2, 3-dihydro-1H-indene-5-carboxamide-based discoidin domain receptors 1 (DDR1) inhibitors: design, synthesis, and in vivo anti-pancreatic cancer efficacy. Journal of Medicinal Chemistry, 62, 7431–7444.

MLA Style

Zhu, D., et al. “2-Amino-2, 3-Dihydro-1H-Indene-5-Carboxamide-Based Discoidin Domain Receptors 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Anti-Pancreatic Cancer Efficacy.” Journal of Medicinal Chemistry, vol. 62, American Chemical Society, 2019, pp. 7431–44.

Chicago Style

Zhu, D, H Huang, D Pinkas, J Luo, D Ganguly, A Fox, E Arner, et al. 2019. “2-Amino-2, 3-Dihydro-1H-Indene-5-Carboxamide-Based Discoidin Domain Receptors 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Anti-Pancreatic Cancer Efficacy.” Journal of Medicinal Chemistry 62: 7431–44.
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Files:: acs.jmedchem.9b00365.pdf

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Publisher copy:: 10.1021/acs.jmedchem.9b00365

Authors

+ Zhu, D More by this author

Role:: Author

+ Huang, H More by this author

Role:: Author

+ Pinkas, D More by this author

Institution:: University of Oxford
Division:: Medical Sciences Division
Department:: NDM
Sub department:: Structural Genomics Consortium
Role:: Author

+ Luo, J More by this author

Role:: Author

+ Ganguly, D More by this author

Role:: Author

More authors...

+ Wellcome Trust More from this funder

Grant:: 106169/Z/14/Z

Publisher:: American Chemical Society
Journal:: Journal of Medicinal Chemistry More from this journal
Volume:: 62
Pages:: 7431-7444
Publication date:: 2019-07-16
Acceptance date:: 2019-07-16
DOI:: 10.1021/acs.jmedchem.9b00365
EISSN:: 1520-4804
ISSN:: 0022-2623

Language:: English
Pubs id:: pubs:1037319
UUID:: uuid:58369c1b-41d3-42c4-8c89-be57ebba3ae4
Local pid:: pubs:1037319
Source identifiers:: 1037319
Deposit date:: 2019-08-02

Terms of use

Copyright holder:: American Chemical Society
Copyright date:: 2019
Notes:: © 2019 American Chemical Society

Licence:: CC Attribution (CC BY)

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