Publications by authors named "Les Dakin"

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Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).
Bin Yang, Alexander W Hird, Michael S Bodnarchuk, Xiaolan Zheng, Les Dakin

Bioorg Med Chem· January 2020

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Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Lakshmaiah Gingipalli, Michael H Block, Larry Bao, Emma Cooke, Les A Dakin

Bioorg Med Chem Lett· May 2018

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Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Rishi G Vaswani, Victor S Gehling, Les A Dakin, Andrew S Cook, Christopher G Nasveschuk

J Med Chem· November 2016

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Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Terry D Crawford, Vickie Tsui, E Megan Flynn, Shumei Wang, Alexander M Taylor, Les A Dakin

J Med Chem· June 2016

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Discovery, design, and synthesis of indole-based EZH2 inhibitors.
Victor S Gehling, Rishi G Vaswani, Christopher G Nasveschuk, Martin Duplessis, Priyadarshini Iyer, Les A Dakin

Bioorg Med Chem Lett· September 2015

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EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.
William D Bradley, Shilpi Arora, Jennifer Busby, Srividya Balasubramanian, Victor S Gehling, Les A Dakin

Chem Biol· November 2014

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A practical synthesis of indoles via a Pd-catalyzed C-N ring formation.
Rishi G Vaswani, Brian K Albrecht, James E Audia, Alexandre Côté, Les A Dakin

Org Lett· August 2014

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AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia.
Erika K Keeton, Kristen McEachern, Keith S Dillman, Sangeetha Palakurthi, Yichen Cao, Les A Dakin

Blood· February 2014

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Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Richard A Ward, Mark J Anderton, Susan Ashton, Paul A Bethel, Matthew Box, Les A Dakin

J Med Chem· September 2013

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Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507.
David A Scott, Les A Dakin, Kevin Daly, David J Del Valle, R Bruce Diebold

Bioorg Med Chem Lett· August 2013

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Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.
Bin Yang, Alexander W Hird, Daniel John Russell, Benjamin P Fauber, Les A Dakin

Bioorg Med Chem Lett· July 2012

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Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Les A Dakin, Michael H Block, Huawei Chen, Erin Code, James E Dowling

Bioorg Med Chem Lett· July 2012

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3-amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor.
David A Scott, Les A Dakin, David J Del Valle, R Bruce Diebold, Lisa Drew

Bioorg Med Chem Lett· March 2011

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Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity.
Paul D Lyne, Brian Aquila, Donald J Cook, Les A Dakin, Jay Ezhuthachan

Bioorg Med Chem Lett· February 2009

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3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile.
David A Scott, Kirsten J Bell, Cheryl T Campbell, Donald J Cook, Les A Dakin

Bioorg Med Chem Lett· February 2009

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Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer.
David A Scott, Brian M Aquila, Geraldine A Bebernitz, Donald J Cook, Les A Dakin

Bioorg Med Chem Lett· September 2008

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[4 + 2]-annulations of chiral organosilanes: Application to the total synthesis of leucascandrolide A.
Qibin Su, Les A Dakin, James S Panek

J Org Chem· January 2007

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Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
Mark Froimowitz, Yonghong Gu, Les A Dakin, Pamela M Nagafuji, Charles J Kelley

J Med Chem· January 2007

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Vinylogous amide analogs of methylphenidate.
Mark Froimowitz, Yonghong Gu, Les A Dakin, Charles J Kelley, Damon Parrish

Bioorg Med Chem Lett· June 2005

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Enantioselective [4 + 2]-annulation of chiral crotylsilanes: application to the synthesis of a C1-C22 fragment of leucascandrolide A.
Les A Dakin, James S Panek

Org Lett· October 2003

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A mild, chemoselective protocol for the removal of thioketals and thioacetals mediated by Dess-Martin periodinane.
Neil F Langille, Les A Dakin, James S Panek

Org Lett· February 2003

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Synthesis of the C1'-C11' oxazole-containing side chain of leucascandrolide A. Application of a Sonogashira cross-coupling.
Les A Dakin, Neil F Langille, James S Panek

J Org Chem· September 2002

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Sonogashira coupling of functionalized trifloyl oxazoles and thiazoles with terminal alkynes: synthesis of disubstituted heterocycles.
Neil F Langille, Les A Dakin, James S Panek

Org Lett· July 2002

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