Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity

Dao, Pascal; Jarray, Rafika; Coq, Johanne Le; Lietha, Daniel; Loukaci, Ali; Lepelletier, Yves; Hadj-Slimane, Réda; Garbay, Christiane; Raynaud, Françoise; Chen, Huixiong

doi:10.1016/j.bmcl.2013.06.038

Cited by 50 publications

(38 citation statements)

References 24 publications

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“…Pass online prediction showed that compound 1 had a predictive activity (Pa) of 0.491 and predicted inactivity (Pi) 0.010 as focal adhesion kinase (FAK) inhibitor. Target Hunter online server showed that compound 1 had score of 0.65 when compared with the recently developed FAK inhibitor 3, Figure …”

Section: Resultsmentioning

confidence: 99%

“…Target Hunter online server showed that compound 1 had score of 0.65 when compared with the recently developed FAK inhibitor 3, Figure 10. 30 Focal adhesion kinase (FAK) is a non-receptor (cytoplasmic) tyrosine kinase. It acts as an intracellular mediator for extracellular events such as matrix remodeling, growth factors, and nutrient availability.…”

Section: Target Prediction and Docking Studymentioning

confidence: 99%

“…Variable amounts of compound 1 solution (25-700 μL) were used; then, 10 μL of Na 131 I was added to a dark screw cap vial. Different volumes of NCS stock solution were added in various amounts (10-200 μL), and the reaction allowed to proceed for various time intervals (15,30,45, and 60 minutes). The radioiodination reaction was kept at ambient temperature, and the pH of the reaction was 5.…”

Section: Studying Factors Affecting the Radiochemical Yieldmentioning

confidence: 99%

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Radioiodination and biological distribution of a new s‐triazine derivative for tumor uptake evaluation

Motaleb

Ibrahim

Sarhan

et al. 2018

Labelled Comp Radiopharmac

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A newly synthesized s-triazine derivative 1,1',1″-(((1,3,5-triazine-2,4,6-triyl) tris (azanediyl)) tris (benzene-4,1-diyl))tris (ethan-1-one), (1), was synthesized as a part of an ongoing research for development of novel s-triazine-based radiopharmaceuticals. In-vitro cell viability assay against different human cancer cell lines showed very promising inhibitory activity of the synthesized compound. This finding encouraged the radioiodination of 1 to study the degree of its localization in tumor site for evaluating the possibility of its use as a tumor imaging agent. The biodistribution study showed good localization of the radioiodinated derivative 2 at tumor site following i.v. administration in solid tumor-bearing mice. Finally, in a trial to understand the mechanism of the anticancer effect exerted by 1, a target prediction study and a docking study were performed. The results of the first study showed that focal adhesion kinase is a possible target for compound 1 and the docking study confirmed successful binding of both compound 1 and its radioiodinated derivative 2 to the binding site of focal adhesion kinase. As a conclusion, the results of this study suggest that, compound 2 could be used as a potential agent for tumor imaging after preclinical trials.

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Section: Resultsmentioning

confidence: 99%

Section: Target Prediction and Docking Studymentioning

confidence: 99%

Section: Studying Factors Affecting the Radiochemical Yieldmentioning

confidence: 99%

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Radioiodination and biological distribution of a new s‐triazine derivative for tumor uptake evaluation

Motaleb

Ibrahim

Sarhan

et al. 2018

Labelled Comp Radiopharmac

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“…As FAK inhibitors, a novel series of diarylamino-1, 3, 5-triazine derivatives ( Figure 10) were reported by Dao et al which demonstrated deleterious effects on endothelial cell viability essentially and the best of our depressants showed a comparable potency on cell activity at significantly low concentration. PHM16 (Figure 10) available inhibited FAK autophosphorylate at in HUVEC cells, indicating it could potently block FAK signaling route in living cells [78].…”

Section: 3 5-triazine Derivatives Targeting Fakmentioning

confidence: 96%

A Systematic Review on Antitumor Agents with 1, 3, 5-triazines

Liu¹

2015

Med chem

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“…Biologically relevant trisubstituted triazines include the antigastric ulcer agent irsogladine, 9 commonly used in Japan and also shown to possess anti-angiogenic/antimetastatic activity; 10 plus other agents with anticancer, 11 antimalarial, 12 antimicrobial 13 and anti-angiogenic 14 properties.…”

Section: Introductionmentioning

confidence: 99%

Optimised synthesis of diamino-triazinylmethyl benzoates as inhibitors of Rad6B ubiquitin conjugating enzyme

Kothayer

Morelli

Brahemi

et al. 2014

Tetrahedron Letters

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Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity

Cited by 50 publications

References 24 publications

Radioiodination and biological distribution of a new s‐triazine derivative for tumor uptake evaluation

Radioiodination and biological distribution of a new s‐triazine derivative for tumor uptake evaluation

A Systematic Review on Antitumor Agents with 1, 3, 5-triazines

Optimised synthesis of diamino-triazinylmethyl benzoates as inhibitors of Rad6B ubiquitin conjugating enzyme

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