Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors

Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors Publisher Pubmed

Dadashpour S^{1, 2} ; Kucukkilinc TT³ ; Ayazgok B³ ; Hosseinimehr SJ⁴ ; Chippindale AM⁵ ; Foroumadi A⁶ ; Irannejad H¹

Source: Future Medicinal Chemistry Published:2019

Abstract

Aim: Mesenchymal-epithelial transition factor (c-Met)/HGF overactivation is involved in diverse human cancers. Materials & methods: Herein, we report the synthesis and biological evaluation of thiomethylpyridine-linked triazolotriazines as c-Met kinase inhibitors. Results: Compounds 10b and 11e were more potent than crizotinib on HepG2 cells with IC50 values of 0.74 and 0.71 μM in the MTT assay, respectively. Interestingly, all of the target compounds displayed IC50 values in the range of 3.9-11.1 nM in the c-Met kinase inhibition assay which were lower than the value for crizotinib (11.1 nM). Conclusion: Target compound 10b can be considered as a leading drug candidate due to its lower IC50 values than crizotinib in both HGF-induced proliferation and c-Met kinase inhibition assays. © 2019 Newlands Press.

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Alireza Foroumadi (9)

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Style	Citing Format
MLA	Dadashpour S, et al.. "Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors." Future Medicinal Chemistry, vol. 11, no. 10, 2019, pp. 1119-1136.
APA	Dadashpour S, Kucukkilinc TT, Ayazgok B, Hosseinimehr SJ, Chippindale AM, Foroumadi A, Irannejad H (2019). Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors. Future Medicinal Chemistry, 11(10), 1119-1136.
Chicago	Dadashpour S, Kucukkilinc TT, Ayazgok B, Hosseinimehr SJ, Chippindale AM, Foroumadi A, Irannejad H. "Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors." Future Medicinal Chemistry 11, no. 10 (2019): 1119-1136.
Harvard	Dadashpour S et al. (2019) 'Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors', Future Medicinal Chemistry, 11(10), pp. 1119-1136.
Vancouver	Dadashpour S, Kucukkilinc TT, Ayazgok B, Hosseinimehr SJ, Chippindale AM, Foroumadi A, et al.. Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors. Future Medicinal Chemistry. 2019;11(10):1119-1136.
BibTex	@article{ author = {Dadashpour S and Kucukkilinc TT and Ayazgok B and Hosseinimehr SJ and Chippindale AM and Foroumadi A and Irannejad H}, title = {Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors}, journal = {Future Medicinal Chemistry}, volume = {11}, number = {10}, pages = {1119-1136}, year = {2019} }
RIS	TY - JOUR AU - Dadashpour S AU - Kucukkilinc TT AU - Ayazgok B AU - Hosseinimehr SJ AU - Chippindale AM AU - Foroumadi A AU - Irannejad H TI - Discovery of Novel 1,2,4-Triazolo-1,2,4-Triazines With Thiomethylpyridine Hinge Binders As Potent C-Met Kinase Inhibitors JO - Future Medicinal Chemistry VL - 11 IS - 10 SP - 1119 EP - 1136 PY - 2019 ER -

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