J. Luengo

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MANIPULATION OF THE RAPAMYCIN EFFECTOR DOMAIN. SELECTIVE NUCLEOPHILIC SUBSTITUTION OF THE C7 METHOXY GROUP

J. Luengo, A. Konialian-Beck, L. Rozamus, 1994 .

Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.

J. F. Mack, J. Luengo, Ramona N Plant, 2012, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of macrocyclic FKBP ligands

J. Luengo, A. Konialian-Beck, D. Holt, 1994 .

Structure-activity studies of synthetic FKBP ligands as peptidyl-prolyl isomerase inhibitors

J. Luengo, A. Konialian-Beck, L. Rozamus, 1994 .

Studies on selective reductions of rapamycin

J. Luengo, L. Rozamus, D. Holt, 1994 .

Efficient removal of pipecolinate from rapamycin and FK506 by reaction with n-Bu4N+CN−

J. Luengo, L. Rozamus, D. Holt, 1993 .

Structure-activity studies of nonmacrocyclic rapamycin derivatives

J. Luengo, D. Holt, A. Badger, 1993 .

In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor

J. Luengo, Mark Cockerill, D. Mcnulty, 2020, Haematologica.

Design, synthesis and evaluation of dual domain FKBP ligands

J. Luengo, D. Holt, A. Badger, 1994 .

Studies on the chemistry of rapamycin: Novel transformations under Lewis-acid catalysis

J. Luengo, D. Holt, Arda L. Konialian, 1993 .

Chapter 9. Endothelin Antagonists

J. D. Elliott, J. Luengo, C. E. Peishoff, 1996 .

Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.

J. Luengo, A. P. Graves, M. Pappalardi, 2019, ACS medicinal chemistry letters.

Pyrido[1,2-a]quinoxalines: synthesis, crystal structure determination and pH-dependent fluorescence

J. Luengo, Hung‐Yuan Cheng, K. Duffy, 2002 .

Pharmacologic characterization of the novel, orally available endothelin-A--selective antagonist SB 247083.

J. D. Elliott, J. Luengo, S. Douglas, 1998, Journal of cardiovascular pharmacology.

Nucleoside protein arginine methyltransferase 5 (PRMT5) inhibitors.

J. Luengo, Hong Lin, 2019, Bioorganic & medicinal chemistry letters.

Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors

J. Luengo, K. Vaddi, Rupa Shetty, 2019, ACS medicinal chemistry letters.

Synthesis of C-fucopyranosyl analogs of GDP-L-fucose as inhibitors of fucosyltransferases

J. Luengo, J. Gleason, 1992 .

Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.

J. F. Mack, J. Luengo, Ramona N Plant, 2012, ACS medicinal chemistry letters.

Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.

J. Luengo, D. Yamashita, D. Heerding, 2009, Bioorganic & medicinal chemistry letters.

[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors.

J. Luengo, Ramona N Plant, K. Erhard, 2013, ACS medicinal chemistry letters.

Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors.

J. Luengo, Ramona N Plant, K. Erhard, 2012, Bioorganic & medicinal chemistry letters.

Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia

Peter A. Jones, Philip J. Chapman, P. Grandi, 2021, Nature Cancer.

An efficient synthesis of 3-substituted 3H-pyrimidin-4-ones.

J. Luengo, D. Yamashita, J. U. Jeong, 2004, Organic letters.

Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis.

J. Luengo, K. Duffy, M. Darcy, 2001, Journal of medicinal chemistry.

The anionic oxy-claisen rearrangement of enolates of .alpha.-allyloxy ketones. A remarkable rate accelerating effect exhibited by the nature of the counterion

J. Luengo, M. Koreeda, M. Koreeda*, 1985 .

Synthesis of (.+-.)-verrucarol using a remarkably facile alumina-catalyzed intramolecular Diels-Alder reaction

J. Luengo, D. Ricca, M. Koreeda, 1988 .

Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules. 2. Rational design of naphtho[1,2-d]imidazole thrombopoietin mimics.

J. Luengo, S. Miller, L. Zhang, 2002, Journal of medicinal chemistry.

Ionization of the c7 methoxy group in rapamycin by 5 M lithium perchlorate-diethyl ether

J. Luengo, A. Konialian-Beck, D. Holt, 1995 .

A novel synthesis of 2-(2-quinoxalino)-3,5-diarylfurans

J. Luengo, A. Konialian-Beck, K. Duffy, 1998 .

Stereospecific synthesis of Z- and E-1 alkoxy-1,3-butadienes

J. Luengo, M. Koreeda, 1984 .

A novel type of intramolecular Diels-Alder reaction involving dienol ethers: an unusual preference for a boat transition state in the incipient ring formation

J. Luengo, M. Koreeda, 1984 .

Complete control of the rearrangement modes of enolates of .alpha.-allyloxy ketones: reversal from the [3,3]-Claisen to the [2,3]-Wittig pathway by the use of the metalated N,N-dimethylhydrazones

J. Luengo, M. Koreeda, 1989 .

Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules. 1. Discovery and optimization of salicylaldehyde thiosemicarbazone thrombopoietin mimics.

J. Luengo, S. Miller, L. Zhang, 2002, Journal of medicinal chemistry.

A small, nonpeptidyl mimic of granulocyte-colony-stimulating factor [see commetns].

J G Gleason, J. Luengo, J. Gleason, 1998, Science.

Selective Binding and Oligomerization of the Murine Granulocyte Colony-stimulating Factor Receptor by a Low Molecular Weight, Nonpeptidyl Ligand*

Michael L Doyle, John Trill, Ruth Lehr, 2003, The Journal of Biological Chemistry.

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.

Kaushik Raha, Dashyant Dhanak, David Sutton, 2010, ACS medicinal chemistry letters.

Preclinical Activity of Eltrombopag (SB-497115), an Oral, Nonpeptide Thrombopoietin Receptor Agonist

J. Luengo, S. Miller, K. Duffy, 2009, Stem cells.

Discovery of SB-497115, a Small-Molecule Thrombopoietin (TPO) Receptor Agonist for the Treatment of Thrombocytopenia.

Stephen G. Miller, Kevin J. Duffy, J. Luengo, 2004 .

Biological Activity and Selectivity for Tpo Receptor of the Orally Bioavailable, Small Molecule Tpo Receptor Agonist, SB-497115.

J. Luengo, S. Miller, K. Duffy, 2004 .

Species Specificity and Receptor Domain Interaction of a Small Molecule TPO Receptor Agonist.

J. Luengo, S. Miller, K. Duffy, 2004 .

In vitro and in vivo biology of a small molecular weight Tpo receptor agonist, SB-497115

J. Luengo, K. Duffy, R. Keenan, 2005 .

Unusual ligand-dependent chemoselective Suzuki–Miyaura cross-coupling reactions of 3-bromo-4-trifloyl-thiophenes

J. Luengo, Jizhou Wang, M. Seefeld, 2011 .

Metal-catalyzed cyclization via isomerization of .alpha.-dienyl-.omega.-allyl acetates

B. Trost, J. Luengo, 1988 .

Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high-affinity and selective nonpeptide ETA receptor antagonist.

J. D. Elliott, J. Luengo, D. Brooks, 1998, The Journal of pharmacology and experimental therapeutics.

Structure-activity studies of rapamycin analogs: evidence that the C-7 methoxy group is part of the effector domain and positioned at the FKBP12-FRAP interface.

J. Luengo, L. Rozamus, D. Yamashita, 1995, Chemistry & biology.

2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.

J. Luengo, D. Yamashita, D. Heerding, 2010, Bioorganic & medicinal chemistry letters.

Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.

Sharad Verma, Kristin K. Brown, Anthony E Choudhry, 2010, Bioorganic & medicinal chemistry letters.

Exploiting Binding-Site Arginines in Drug Design: Recent Examples.

J. Luengo, Hong Lin, 2020, Bioorganic & medicinal chemistry letters.

Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.

Yong Jiang, Jacques Briand, Junya Qu, 2016, ACS medicinal chemistry letters.

Benzophenone- and indolecarboxylic acids: potent type-2 specific inhibitors of human steroid 5 alpha-reductase.

J. Luengo, A. Konialian-Beck, D. Holt, 1995, Journal of medicinal chemistry.

2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.

Kristin K. Brown, J. Luengo, Rakesh Kumar, 2010, Bioorganic & medicinal chemistry letters.

DESIGN, SYNTHESIS, AND KINETIC EVALUATION OF HIGH-AFFINITY FKBP LIGANDS AND THE X-RAY CRYSTAL-STRUCTURES OF THEIR COMPLEXES WITH FKBP12.

Jon Clardy, J. Luengo, L. Rozamus, 1994 .

Molecular clinical safety intelligence: a system for bridging clinically focused safety knowledge to early-stage drug discovery - the GSK experience.

Darren V S Green, Dana E Vanderwall, David Fram, 2011, Drug discovery today.

Nuisance Compounds, PAINS Filters, and Dark Chemical Matter in the GSK HTS Collection

Stephen D Pickett, Darren V S Green, Subhas J Chakravorty, 2018, SLAS discovery : advancing life sciences R & D.

Yin and Yang in medicinal chemistry: what does drug-likeness mean?

Ricardo Macarrón, J. Luengo, Juan I Luengo, 2011, Future medicinal chemistry.

Plasma- and cerebrospinal fluid-immunoreactive endothelin-1: effects of nonpeptide endothelin receptor antagonists with diverse affinity profiles for endothelin-A and endothelin-B receptors.

J. D. Elliott, J. Luengo, R. Willette, 1998, Journal of cardiovascular pharmacology.