Výsledky vyhledávání - "Marc I Broudy"

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR–ABL including the T315I gatekeeper mutant

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:3743-3748

Ponatinib (AP24534) was previously identified as a pan-BCR-ABL inhibitor that potently inhibits the T315I gatekeeper mutant, and has advanced into clinical development for the treatment of refractory or resistant CML. In this study, we explored a nov

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66a38549836ca328c6bb343c0b0ec0da
https://doi.org/10.1016/j.bmcl.2011.04.060

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Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

Publikováno v: Journal of Medicinal Chemistry. 53:4701-4719

In the treatment of chronic myeloid leukemia (CML) with BCR-ABL kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently approved agents. This report describes the structure-guided design of a novel series of potent pa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::757a483ca43d6a44106283733dc26b6a
https://doi.org/10.1021/jm100395q

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9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation

Publikováno v: Journal of Medicinal Chemistry. 52:4743-4756

A novel series of potent dual Src/Abl kinase inhibitors based on a 9-(arenethenyl)purine core has been identified. Unlike traditional dual Src/Abl inhibitors targeting the active enzyme conformation, these inhibitors bind to the inactive, DFG-out con

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15c4c8fc144dc20cf0e38dd91c2a9789
https://doi.org/10.1021/jm900166t

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HIGHLY SELECTIVE INHIBITION OF HUMAN CYP3A IN VITRO BY AZAMULIN AND EVIDENCE THAT INHIBITION IS IRREVERSIBLE

Autor: John C. L. Erve, Charles L. Crespi, Stephanie D. Turner, Andrew P. Blanchard, David M. Stresser, Christopher J. Patten, Raman Sharma, Catherine E. Cargill, Marc I. Broudy, Thuy Ho, Joseph J. Goodwin, Andre A. Dandeneau, Shangara S. Dehal

Publikováno v: Drug Metabolism and Disposition. 32:105-112

Azamulin [14-O-(5-(2-amino-1,3,4-triazolyl)thioacetyl)-dihydromutilin] is an azole derivative of the pleuromutilin class of antiinfectives. We tested the inhibition potency of azamulin toward 18 cytochromes P450 using human liver microsomes or micros

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b3591095bd3827c7d53a82bd20d40b4
https://doi.org/10.1124/dmd.32.1.105

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Quantification of 9-Carboxy-11-nor-Δ9-tetrahydrocannabinol in Urine Using Brominated 9-Carboxy-11-nor-Δ9-tetrahydrocannabinol as the Internal Standard and High-Performance Liquid Chromatography with Electrochemical Detection

Autor: Daniel H. Fisher, L. Megan Fisher, Marc I. Broudy

Publikováno v: Biomedical Chromatography. 10:161-166

A method was developed for quantitating 9-carboxy-11-nor-delta 9-tetrahydrocannabinol in human urine as part of the process for validating an automated enzyme immunoassay for marijuana metabolites. Sample cleanup was accomplished using a mixed-mode s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c2d5d72759fe43fd0eaee7745f552e7f
https://doi.org/10.1002/(sici)1099-0801(199607)10:4<161::aid-bmc579>3.0.co

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Evaluation of Four Methods for Catecholamine Analysis in Plasma Obtained From Subjects During Incremental Cycle Ergometry

Autor: Marc I. Broudy, Daniel H. Fisher, L. Megan Fisher

Publikováno v: Journal of Liquid Chromatography. 18:3311-3327

Plasma was collected from a subject during incremental cycle ergometry in order to determine the anaerobic threshold. Norepinephrine and epinephrine were extracted using alumina, strong-cation exchange/alumina, or weak-cation exchange, and then separ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b9368e198c74ab2810a47bde2bb7dda3
https://doi.org/10.1080/10826079508010453

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Akademický článek

9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation.

Publikováno v: Journal of Medicinal Chemistry; Aug2009, Vol. 52 Issue 15, p4743-4756, 14p

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