Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors
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Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors
| Title: | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors |
| Author: |
Sim, Taebo; Sasaki, Takaaki; Luther, William; Deng, Xianming; Wang, Jinhua; Zhang, Jianming; Kim, Nam Doo; George, Rani E.; Jänne, Pasi A.; Gray, Nathanael Schiander
Note: Order does not necessarily reflect citation order of authors. |
| Citation: | Deng, Xianming, Jinhua Wang, Jianming Zhang, Taebo Sim, Nam Doo Kim, Takaaki Sasaki, William Luther, Rani E. George, Pasi A. Jänne, and Nathanael S. Gray. 2011. Discovery of 3,5-diamino-1,2,4-triazole ureas as potent anaplastic lymphoma kinase inhibitors. ACS Medicinal Chemistry Letters 2(5): 379-384. |
| Full Text & Related Files: |
3093683.pdf (1.187Mb; PDF) 
|
| Abstract: | A series of novel 3,5-diamino-1,2,4-triazole benzyl ureas was identified as having potent anaplastic lymphoma kinase (ALK) inhibition exemplified by 15a, 20a, and 23a, which exhibited antiproliferative IC50 values of 70, 40, and 20 nM in Tel-ALK transformed Ba/F3 cells, respectively. Moreover, 15a and 23a potently inhibited the growth and survival of NPM-ALK positive anaplastic large cell lymphoma cell (SU-DHL-1) and neuroblastoma cell lines (KELLY, SH-SY5Y) containing the F1174L ALK mutation. These compounds provide novel leads for the development of small-molecule ALK inhibitors for cancer therapy. |
| Published Version: | doi://10.1021/ml200002a |
| Other Sources: | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3093683/pdf/ |
| Terms of Use: | This article is made available under the terms and conditions applicable to Other Posted Material, as set forth at http://nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of-use#LAA |
| Citable link to this page: | http://nrs.harvard.edu/urn-3:HUL.InstRepos:5978752 |
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