Výsledky vyhledávání - "Karin Russian"

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

Zobrazit plný text záznamu

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

Zobrazit plný text záznamu

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

Zobrazit plný text záznamu

Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors

Publikováno v: Bioorganicmedicinal chemistry letters. 18(17)

Novel N(9)-arenethenyl purines, optimized potent dual Src/Abl tyrosine kinase inhibitors, are described. The key structural feature is a trans vinyl linkage at N(9) on the purine core which projects hydrophobic substituents into the selectivity pocke

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5da3a1390a4f7a4e52e9c0e9b83b4093
https://pubmed.ncbi.nlm.nih.gov/18691885

Zobrazit plný text záznamu

Potent Antitumor Activity of AP24534, an Orally Active Inhibitor of Bcr-Abl Variants Including T315I, in In Vitro and In Vivo Models of Chronic Myeloid Leukemia (CML)

Autor: Scott Wardwell, Thomas O'Hare, Tim Clackson, Brian J. Druker, Jeffrey Keats, Qihong Xu, Karin Russian, Victor M. Rivera, John D. Iuliucci, Joseph Snodgrass, Yaoyu Ning, William C. Shakespeare, Amie S. Corbin, Sarah Lamore, Marc Broudy, Frank Wang

Publikováno v: Blood. 110:1032-1032

Resistance to current Bcr-Abl kinase inhibitors in CML patients is associated with the emergence of Bcr-Abl point mutations, including the T315I variant which represents 15–20% of clinically observed mutants and is resistant to all approved agents

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::31c95b19df84b8f1952d2e35a94e93bc
https://doi.org/10.1182/blood.v110.11.1032.1032

Zobrazit plný text záznamu

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

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání