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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.
Bioorg Med Chem Lett; 21(24): 7325-30, 2011 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-22041060
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 novel series of potent JAK2 inhibitors containing a 2,7-pyrrolotriazine core. To minimize potential drug-induced toxicity, targets were analyzed for the ability to form a glutathione adduct. Glutathione adduct formation was decreased by modification of the aniline substituent at C2.
Selo DaSilva