1233141-91-7Relevant academic research and scientific papers
2,7-Disubstituted-pyrrolo[2,1- f ][1,2,4]triazines: New variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity
Ott, Gregory R.,Wells, Gregory J.,Thieu, Tho V.,Quail, Matthew R.,Lisko, Joseph G.,Mesaros, Eugen F.,Gingrich, Diane E.,Ghose, Arup K.,Wan, Weihua,Lu, Lihui,Cheng, Mangeng,Albom, Mark S.,Angeles, Thelma S.,Huang, Zeqi,Aimone, Lisa D.,Ator, Mark A.,Ruggeri, Bruce A.,Dorsey, Bruce D.
, p. 6328 - 6341 (2011/11/12)
A novel 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazine scaffold has been designed as a new kinase inhibitor platform mimicking the bioactive conformation of the well-known diaminopyrimidine motif. The design, synthesis, and validation of this new pyrrolo[2,1-f][1,2,4]triazine scaffold will be described for inhibitors of anaplastic lymphoma kinase (ALK). Importantly, incorporation of appropriate potency and selectivity determinants has led to the discovery of several advanced leads that were orally efficacious in animal models of anaplastic large cell lymphoma (ALCL). A lead inhibitor (30) displaying superior efficacy was identified and in depth in vitro/in vivo characterization will be presented.
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: Modification of target structure to minimize reactive metabolite formation
Weinberg, Linda R.,Albom, Mark S.,Angeles, Thelma S.,Breslin, Henry J.,Gingrich, Diane E.,Huang, Zeqi,Lisko, Joseph G.,Mason, Jennifer L.,Milkiewicz, Karen L.,Thieu, Tho V.,Underiner, Ted L.,Wells, Gregory J.,Wells-Knecht, Kevin J.,Dorsey, Bruce D.
, p. 7325 - 7330 (2012/02/04)
The JAK2/STAT pathway has important roles in hematopoiesis. With the discovery of the JAK2 V617F mutation and its presence in many patients with myeloproliferative neoplasms, research in the JAK2 inhibitor arena has dramatically increased. We report a nov
