L. Lombardo

发表

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Journal of medicinal chemistry.

The Antiangiogenic Activity in Xenograft Models of Brivanib, a Dual Inhibitor of Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinases

J. Fargnoli, J. Barrish, J. Hunt, 2010, Molecular Cancer Therapeutics.

Assessing compound binding to the Eg5 motor domain using a thermal shift assay.

M. Doyle, V. Goldfarb, W. Metzler, 2009, Analytical biochemistry.

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.

J. Fargnoli, J. Barrish, J. Tokarski, 2005, Journal of medicinal chemistry.

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.

Punit Marathe, Ravindra Tejwani, Arvind Mathur, 2008, Bioorganic & medicinal chemistry letters.

Metabolism of 5-Isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): Identification of an Unusual N-Acetylglucosamine Conjugate in the Cynomolgus Monkey

Y. Shu, Donna D Wei, L. Qian, 2008, Drug Metabolism and Disposition.

Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215)

J. Fargnoli, G. Derbin, J. Barrish, 2008, Journal of medicinal chemistry.

9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.

J. Tokarski, G. Trainor, J. Sack, 2015, Bioorganic & medicinal chemistry letters.

Janus Kinase 2 (JAK2) Inhibitors for the Treatment of Myeloproliferative Neoplasm (MPN)

M. Lorenzi, A. Purandare, L. Lombardo, 2010 .

Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.

J. Tokarski, B. Koplowitz, J. Hunt, 2005, Bioorganic & medicinal chemistry letters.

Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.

J. Fargnoli, J. Tokarski, G. Trainor, 2010, Bioorganic & medicinal chemistry letters.

Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.

David S. Nirschl, David S Nirschl, J. Fargnoli, 2008, Bioorganic & medicinal chemistry letters.

Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.

J. Fargnoli, J. Tokarski, J. Hunt, 2008, Bioorganic & medicinal chemistry letters.

The identification and optimization of orally efficacious, small molecule VLA-4 antagonists.

D. Huryn, S. Ashwell, T. Yednock, 2004, Current topics in medicinal chemistry.

Pulmonary antiallergic and antiinflammatory effects of a novel, orallyactive phosphodiesterase IV inhibitor (WAY-127093B) in guinea pigs and rats

L. Lombardo, D. E. Howell, E. Rubin, 1995, Inflammation Research.

Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.

L. Mueller, S. Sheriff, David K. Williams, 2006, Bioorganic & medicinal chemistry letters.

In Vitro Cardiotoxicity Potential Comparative Assessments of Chronic Myelogenous Leukemia Tyrosine Kinase Inhibitor Therapies: Dasatinib, Imatinib and Nilotinib.

V. Sasseville, F. Lee, M. Slade, 2007 .

Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).

S. Spergel, K. McIntyre, J. Tokarski, 2019, Journal of medicinal chemistry.

The Crystal Structure of Abl Kinase with BMS-354825, a Dual SRC/ABL Kinase Inhibitor.

J. Tokarski, K. Kish, H. Klei, 2004 .

Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.

Robert T. Taylor, A. Polonskaia, M. Weisel, 2013, Journal of medicinal chemistry.

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2

P. Ross-Macdonald, K. McIntyre, G. Trainor, 2012, Leukemia.

Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.

A. Polonskaia, M. Weisel, C. Lukacs, 2013, Journal of medicinal chemistry.

BMS-354825 potently inhibits multiple selected oncogenic tyrosine kinases and possesses broad-spectrum antitumor activities in vitro and in vivo

F. Lee, C. Fairchild, R. Borzilleri, 2005 .

Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.

J. Fargnoli, J. Tokarski, G. Trainor, 2009, Journal of medicinal chemistry.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

S. Spergel, K. McIntyre, D. Shuster, 2019, Journal of medicinal chemistry.

Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.

J. Fargnoli, J. Tokarski, D. Xie, 2008, Journal of medicinal chemistry.

One-pot two step synthesis of 5-cyano-dihydropyrimidinones using polyphosphate ester

David K. Williams, R. Schmidt, L. Lombardo, 2008 .

Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.

Becky Penhallow, Andrew Tebben, Jonathan Lippy, 2012, Bioorganic & medicinal chemistry letters.

Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.

James Lin, K. McIntyre, J. Tokarski, 2019, ACS medicinal chemistry letters.

Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.

David K Williams, Patricia C Weber, D. Chakrabarti, 2005, Journal of medicinal chemistry.

One‐Pot Two Step Synthesis of 5‐Cyano‐dihydropyrimidinones Using Polyphosphate Ester.

David K. Williams, R. Schmidt, L. Lombardo, 2008 .

The chemistry of vicinal tricarbonyls. A stable vinyl tricarbonyl hydrate as a di- and trielectrophile

V. Rotello, N. Murugesan, H. Wasserman, 1989 .

The chemistry of vicinal tricarbonyls a total synthesis of prodigiosin

H. Wasserman, L. Lombardo, 1989 .

Efficacy, Pharmacokinetics, and Metabolism of Tetrahydroquinoline Inhibitors of Plasmodium falciparum Protein Farnesyltransferase

D. Chakrabarti, M. Gelb, F. Buckner, 2007, Antimicrobial Agents and Chemotherapy.

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

J. Fargnoli, G. Derbin, J. Barrish, 2006, Journal of medicinal chemistry.

Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.

D. Chakrabarti, M. Gelb, F. Buckner, 2007, Journal of medicinal chemistry.

Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.

Wayne Vaccaro, Steven Sheriff, Neil Burford, 2006, Bioorganic & medicinal chemistry letters.

Pharmacodynamic analysis of target inhibition and tumor endothelial cell death in biopsies obtained from patients treated with the VEGF receptor antagonists SU5416 or SU6668

F. Lee, N. Donato, M. Talpaz, 2004 .

The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants.

M. Wittekind, J. Tokarski, K. Kish, 2006, Cancer research.

Apoptotic and Cytostatic Farnesyltransferase Inhibitors Have Distinct Pharmacology and Efficacy Profiles in Tumor Models

J. Hunt, F. Lee, V. Manne, 2004, Cancer Research.

Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.

David S. Nirschl, Jonathan Lippy, John S Tokarski, 2011, Bioorganic & medicinal chemistry letters.

BMS-354825, a Dual SRC/ABL Kinase Inhibitor, Displays Potent Anti-Tumor Activity in a Model of Intracranial CML Growth.

F. Lee, R. Borzilleri, F. Luo, 2004 .

Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.

James Lin, K. McIntyre, D. Shuster, 2020, Journal of medicinal chemistry.

Long-Acting Tumor-Activated Prodrug of a TGFβR Inhibitor.

M. Poss, D. Tortolani, R. Borzilleri, 2021, Journal of medicinal chemistry.

Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.

Andrew Tebben, Jonathan Lippy, Michele Modugno, 2012, Bioorganic & medicinal chemistry letters.

Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.

J. Tokarski, G. Trainor, J. Sack, 2015, ACS medicinal chemistry letters.

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

J. Tokarski, G. Trainor, A. Mathur, 2015, ACS medicinal chemistry letters.

Identification of potent tricyclic prodrug S1P1 receptor modulators.

K. McIntyre, D. Shen, A. Mathur, 2017, MedChemComm.

Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors.

Derek J. Norris, D. Shen, G. Trainor, 2015, ACS medicinal chemistry letters.

Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.

J. Fargnoli, G. Derbin, J. Barrish, 2006, Journal of medicinal chemistry.

J. Fargnoli, J. Tokarski, G. Trainor, 2009, Journal of medicinal chemistry.

J. Fargnoli, G. Derbin, J. Barrish, 2008, Bioorganic & medicinal chemistry letters.

Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.

J. Fargnoli, J. Tokarski, J. Hunt, 2008, Bioorganic & medicinal chemistry letters.

Y. Shu, L. Qian, A. Kamath, 2008, Drug Metabolism and Disposition.

Dasatinib (BMS-354825) Overcomes Multiple Mechanisms of Imatinib Resistance in Chronic Myeloid Leukemia (CML).

F. Lee, R. Borzilleri, L. Lombardo, 2005 .

Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.

D. Chakrabarti, F. Buckner, C. Verlinde, 2007, Journal of medicinal chemistry.

Pharmacokinetics- and Pharmacodynamics-Guided Optimization of the Dose and Treatment Schedule for the Dual SRC/ABL Inhibitor BMS-354825.

F. Lee, R. Borzilleri, F. Luo, 2004 .

Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).

S. Spergel, K. McIntyre, J. Tokarski, 2019, Journal of medicinal chemistry.