Did you mean: T. H. E. Magic

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

…, J Xue, H Zhang, A Oleksijew, TJ Magoc… - Science translational …, 2015 - science.org
The BCL-2/BCL-X L /BCL-W inhibitor ABT-263 (navitoclax) has shown promising clinical activity
in lymphoid malignancies such as chronic lymphocytic leukemia. However, its efficacy in …

Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor

DH Albert, P Tapang, TJ Magoc, LJ Pease… - Molecular cancer …, 2006 - AACR
ABT-869 is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor
of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth …

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent …

…, D Wilcox, DH Albert, TJ Magoc… - Journal of medicinal …, 2017 - ACS Publications
The development of bromodomain and extraterminal domain (BET) bromodomain inhibitors
and their examination in clinical studies, particularly in oncology settings, has garnered …

Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744) …

…, L Zhang, Y Shen, DH Albert, TJ Magoc… - Journal of Medicinal …, 2020 - ACS Publications
The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains
two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under …

Fragment-based, structure-enabled discovery of novel pyridones and pyridone macrocycles as potent bromodomain and extra-terminal domain (BET) family …

…, R Hubbard, CH Park, L Li, TJ Magoc… - Journal of medicinal …, 2017 - ACS Publications
Members of the BET family of bromodomain containing proteins have been identified as
potential targets for blocking proliferation in a variety of cancer cell lines. A two-dimensional …

α-Keto amides as inhibitors of histone deacetylase

…, SS Murphy, JJ Bouska, P Tapang, TJ Magoc… - Bioorganic & medicinal …, 2003 - Elsevier
α-Keto ester and amides were found to be potent inhibitors of histone deacetylase.
Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular …

Selective inhibition of the second bromodomain of BET family proteins results in robust antitumor activity in preclinical models of acute myeloid leukemia

…, G Mehta, SS Shanmugavelandy, TJ Magoc… - Molecular cancer …, 2021 - AACR
Dual bromodomain BET inhibitors that bind with similar affinities to the first and second
bromodomains across BRD2, BRD3, BRD4, and BRDT have displayed modest activity as …

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases

…, DH Albert, JJ Bouska, KB Glaser, TJ Magoc… - Bioorganic & medicinal …, 2011 - Elsevier
In an effort to discover Aurora kinase inhibitors, an HTS hit revealed an amide containing
pyrrolopyrimidine compound. Replacement of the pyrrolopyrimidine residue with a …

The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors

…, HR Heyman, JH Holms, DH Albert, TJ Magoc… - Bioorganic & Medicinal …, 1998 - Elsevier
A series of succinate-derived hydroxamic acids incorporating a macrocyclic ring were
designed, synthesized, and evaluated as inhibitors of matrix metalloproteinases. The inhibitors …

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families

…, PA Marcotte, LJ Pease, KB Glaser, TJ Magoc… - Bioorganic & medicinal …, 2012 - Elsevier
In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity,
a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was …
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