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Your search keyword '"Lu, Lihui"' showing total 2 results
2 results on '"Lu, Lihui"'

1. Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

Author

Mesaros, Eugen F., Angeles, Thelma S., Albom, Mark S., Wagner, Jason C., Aimone, Lisa D., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Olsen, Mark, Kordwitz, Emily, Haltiwanger, R. Curtis, Landis, Amy J., Cheng, Mangeng, Ruggeri, Bruce A., Ator, Mark A., Dorsey, Bruce D., and Ott, Gregory R.

Subjects
*PIPERIDINE derivatives, *TRIAZINES, *CHEMICAL inhibitors, *ANAPLASTIC lymphoma kinase, *PHARMACOKINETICS, *STEREOCHEMISTRY
Abstract

The diastereoselective synthesis and biological activity of piperidine-3,4-diol and piperidine-3-ol-derived pyrrolotriazine inhibitors of anaplastic lymphoma kinase (ALK) are described. Although piperidine-3,4-diol and piperidine-3-ol derivatives showed comparable in vitro ALK activity, the latter subset of inhibitors demonstrated improved physiochemical and pharmacokinetic properties. Furthermore, the stereochemistry of the C3 and C4 centers had a marked impact on the in vivo inhibition of ALK autophosphorylation. Thus, trans -4-aryl-piperidine-3-ols ( 22 ) were more potent than the cis diastereomers ( 20 ). [ABSTRACT FROM AUTHOR]

Published
2015
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2. Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models

Author

Mesaros, Eugen F., Burke, Jason P., Parrish, Jonathan D., Dugan, Benjamin J., Anzalone, Andrew V., Angeles, Thelma S., Albom, Mark S., Aimone, Lisa D., Quail, Matthew R., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng, Ott, Gregory R., and Dorsey, Bruce D.

Subjects
*AZEPINES, *PYRIMIDINES, *ANTINEOPLASTIC agents, *DRUG efficacy, *LYMPHOMAS, *ENZYME inhibitors, *LABORATORY mice, *DRUG bioavailability
Abstract

Abstract: The synthesis and biological evaluation of potent and selective anaplastic lymphoma kinase (ALK) inhibitors from a novel class of 2,4-diaminopyrimidines, incorporating 2,3,4,5-tetrahydro-benzo[d]azepine fragments, is described. An orally bioavailable analogue (18) that displayed antitumor efficacy in ALCL xenograft models in mice was identified and extensively profiled. [Copyright &y& Elsevier]

Published
2011
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