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Your search keyword '"Gingrich, Diane E."' showing total 4 results
Start Over Author "Gingrich, Diane E." Publisher elsevier b.v.
4 results on '"Gingrich, Diane E."'

1. Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases

Author

Zificsak, Craig A., Gingrich, Diane E., Breslin, Henry J., Dunn, Derek D., Milkiewicz, Karen L., Theroff, Jay P., Thieu, Tho V., Underiner, Ted L., Weinberg, Linda R., Aimone, Lisa D., Albom, Mark S., Mason, Jennifer L., Saville, Lisa, Husten, Jean, Angeles, Thelma S., Finn, James P., Jan, Mahfuza, O’Kane, Teresa M., Dobrzanski, Pawel, and Dorsey, Bruce D.

Subjects
*PROTEIN-tyrosine kinases, *FOCAL adhesion kinase, *MATHEMATICAL optimization, *CELLULAR signal transduction, *TISSUE scaffolds, *CANCER cells, *TUMOR growth
Abstract

Abstract: The elaboration of a novel scaffold for the inhibition of JAK2 and FAK kinases was targeted in order to provide a dual inhibitor that could target divergent pathways for tumor cell progression. [Copyright &y& Elsevier]

Published
2012
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2. Synthesis and kinase inhibitory activity of 3′-(S)-epi-K-252a

Author

Gingrich, Diane E. and Hudkins, Robert L.

Subjects
*DIASTEREOISOMERS, *PROTEIN-tyrosine kinases
Abstract

The 3′-epi diastereomer of K-252a was synthesized with the goal of evaluating the stereochemical requirements of the 3′-sugar alcohol on kinase inhibitory activity. Inverting the 3′-alcohol resulted in a 20 nM inhibitor of VEGFR2 and a 1 nM inhibitor of TrkA tyrosine kinase. [Copyright &y& Elsevier]

Published
2002
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4. 2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: Modification of target structure to minimize reactive metabolite formation

Author

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., and Dorsey, Bruce D.

Subjects
*PROTEIN-tyrosine kinase inhibitors, *TRIAZINES, *METABOLITES, *TARGETED drug delivery, *CELLULAR signal transduction, *HEMATOPOIESIS, *GENETIC mutation
Abstract

Abstract: 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. [Copyright &y& Elsevier]

Published
2011
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