R. Borzilleri

发表

Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form

Micah T. Nelp, J. Groves, J. Hunt, 2018, Proceedings of the National Academy of Sciences.

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 discovery of macrocyclic XIAP antagonists from a DNA-programmed chemistry library, and their optimization to give lead compounds with in vivo antitumor activity.

Shana L. Posy, J. Fargnoli, R. Talbott, 2015, Journal of medicinal chemistry.

Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.

J. Fargnoli, S. Sheriff, A. Mathur, 2020, ACS medicinal chemistry letters.

Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.

J. Fargnoli, S. Sheriff, B. Fink, 2018, ACS medicinal chemistry letters.

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.

Building homogeneous time-resolved fluorescence resonance energy transfer assays for characterization of bivalent inhibitors of an inhibitor of apoptosis protein target.

Shana L. Posy, W. Metzler, R. Talbott, 2016, Analytical biochemistry.

Recent advances in the discovery and development of antibody – drug conjugates have led to FDA approvals and a rich clinical pipeline of promising new cancer therapies . Antibody – drug conjugates : current status and future directions

R. Borzilleri, P. Cardarelli, G. Vite, 2013 .

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.

Pharmacodynamics‐based approach for efficacious human dose projection of BMS‐986260, a small molecule transforming growth factor beta receptor 1 inhibitor

Y. Shu, R. Borzilleri, M. Cvijic, 2020, Biopharmaceutics & drug disposition.

JAK Family Inhibitors for Autoimmune Diseases

J. Tokarski, R. Borzilleri, Stephen T. Wrobleski, 2021 .

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.

Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGF beta RI).

Amol G. Dikundwar, J. Fargnoli, S. Sheriff, 2018 .

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

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

Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates.

A. Mathur, B. Warrack, A. Rajpal, 2020, Journal of medicinal chemistry.

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

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

Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists.

Shana L. Posy, R. Talbott, S. Emanuel, 2014, Bioorganic & medicinal chemistry letters.

Chapter 15 Case History: Discovery of Ixabepilone (IXEMPRATM), a First-in-Class Epothilone Analog for Treatment of Metastatic Breast Cancer

R. Borzilleri, G. Vite, 2009 .

Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.

Kimberly A. Foster, J. Fargnoli, J. Hunt, 2021, ACS medicinal chemistry letters.

Pharmacology of smac mimetics; chemotype differentiation based on physical association with caspase regulators and cellular transport.

J. Fargnoli, R. Talbott, J. Hunt, 2015, Experimental cell research.

Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.

Shana L. Posy, J. Fargnoli, R. Talbott, 2015, ACS medicinal chemistry letters.

Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity.

J. Fargnoli, R. Talbott, S. Emanuel, 2015, Journal of medicinal chemistry.

Ultrasensitive quantitative LC-MS/MS of an inhibitor of apoptosis protein's antagonist in plasma using protein target affinity extraction.

R. Talbott, R. Borzilleri, T. Olah, 2016, Bioanalysis.

HTRF assays for characterization of bivalent inhibitors of an Inhibitor of Apoptosis Protein target

Shana L. Posy, W. Metzler, R. Talbott, 2015 .

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

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

Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads.

R. Borzilleri, A. Tebben, Yong Zhang, 2017, Bioorganic & medicinal chemistry letters.

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 the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.

J. Fargnoli, J. Hunt, B. Fink, 2004, Journal of medicinal chemistry.

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.

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.

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

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

Imino Ene Reactions in Organic Synthesis

R. Borzilleri, Steven M. Weinreb, S. Weinreb, 1995 .

.beta.-Tosylethylamine: A Useful Reagent for Preparation of N-Protected Amides, Carbamates, and Related Compounds. Application to Synthesis of .beta.-Lactams

R. Borzilleri, S. Weinreb, D. Dipietro, 1994 .

Synthesis and biological activity of novel epothilone aziridines.

C. Fairchild, R. Borzilleri, F. Lee, 2001, Organic letters.

A new method for preparation of 3,6-dihydro-2H-1,3-oxazines and explorations of their use in stereoselective synthesis of 1,3-amino alcohol derivatives

R. Borzilleri, M. Parvez, S. Weinreb, 1996 .

Bis[N‐(p‐toluenesulfonyl)]sulfodiimide

R. Borzilleri, S. Weinreb, 2001 .

N‐Sulfinyl‐p‐toluenesulfonamide

R. Borzilleri, S. Weinreb, 2001 .

Development of a Scalable Synthesis of the Small Molecule TGFβR1 Inhibitor BMS-986260

David K. Leahy, Martin D. Eastgate, A. Mathur, 2020 .

Total Synthesis of the Unusual Marine Alkaloid (-)-Papuamine Utilizing a Novel Imino Ene Reaction

R. Borzilleri, M. Parvez, S. Weinreb, 1995 .

Total synthesis of papuamine via a stereospecific intramolecular imino ene reaction of an allenylsilane

R. Borzilleri, M. Parvez, S. Weinreb, 1994 .

Rearrangements of some furan and banzofuran 1.5,-dienols

R. Borzilleri, David Martin, M. Boylan, 1993 .

A Novel Application of a Pd(0)-Catalyzed Nucleophilic Substitution Reaction to the Regio- and Stereoselective Synthesis of Lactam Analogues of the Epothilone Natural Products

Soong-Hoon Kim, C. Fairchild, R. Borzilleri, 2000 .

SYNTHESIS OF THE VANCOMYCIN CD AND DE RING SYSTEMS

D. Boger, R. Borzilleri, R. Beresis, 1997 .

An unusually facile SnAr 14-membered biaryl ether macrocyclization reaction suitable for preparation of the cycloisodityrosine subunit of bouvardin, deoxybouvardin and related agents

D. Boger, R. Borzilleri, 1995 .

Synthesis of appropriately functionalized vancomycin CD and DE ring systems

D. Boger, R. Borzilleri, S. Nukui, 1995 .

Preclinical discovery of ixabepilone, a highly active antineoplastic agent

F. Lee, A. Kamath, C. Fairchild, 2008, Cancer Chemotherapy and Pharmacology.

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.

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.

J. Fargnoli, J. Tokarski, J. Hunt, 2005, Bioorganic & medicinal chemistry letters.

An innovative kinome platform to accelerate small-molecule inhibitor discovery and optimization from hits to leads.

J. Tokarski, R. Borzilleri, W. Pitts, 2021, Drug discovery today.

Decarboxylative Peptide Macrocyclization through Photoredox Catalysis.

Martin D. Eastgate, M. Poss, R. Borzilleri, 2017, Angewandte Chemie.

BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy.

F. Lee, Soong-Hoon Kim, C. Fairchild, 2001, Clinical cancer research : an official journal of the American Association for Cancer Research.

Antroquinonol A: Scalable Synthesis and Preclinical Biology of a Phase 2 Drug Candidate

Phil S Baran, J. Fargnoli, R. Borzilleri, 2015, ACS central science.

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 .

Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.

Michael G. Yang, D. Shuster, C. Weigelt, 2021, ACS medicinal chemistry letters.

Mcl-1 antagonism is a potential therapeutic strategy in a subset of solid cancers.

M. Modugno, D. Ballinari, W. Pastori, 2015, Experimental cell research.

Antibody-drug conjugates: current status and future directions.

R. Borzilleri, P. Cardarelli, G. Vite, 2014, Drug discovery today.

Synthesis of (9R,12S)- and (9S,12S)-Cycloisodityrosine and Their N-Methyl Derivatives.

D. Boger, R. Borzilleri, Jiacheng Zhou, 1997, The Journal of organic chemistry.

Synthesis of (9R,12S)‐ and (9S,12S)‐Cycloisodityrosine and Their N‐ Methyl Derivatives.

D. Boger, R. Borzilleri, Jiacheng Zhou, 1997 .

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 .

TGFβ2 and TGFβ3 mediate appropriate context-dependent phenotype of rat valvular interstitial cells

Faye Wang, R. Borzilleri, Minxue Huang, 2021, iScience.

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.

Synthesis of (9S,12S)-cycloisodityrosine and its unnatural (9R,12S)-diastereomer

D. Boger, R. Borzilleri, Jiacheng Zhou, 1996 .

Synthesis of (R)-(4-Methoxy-3,5-dihydroxyphenyl)glycine Derivatives: The Central Amino Acid of Vancomycin and Related Agents

D. Boger, R. Borzilleri, S. Nukui, 1996 .

Synthesis of (R)‐(4‐Methoxy‐3,5‐dihydroxyphenyl)glycine Derivatives: The Central Amino Acid of Vancomycin and Related Agents.

D. Boger, R. Borzilleri, S. Nukui, 1996 .

Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).

Amol G. Dikundwar, J. Fargnoli, S. Sheriff, 2018, Bioorganic & medicinal chemistry.

Epothilones: new tubulin polymerization agents in preclinical and clinical development

R. Borzilleri, G. Vite, 2002 .

Highly Efficient Semisynthesis of Biologically Active Epothilone Derivatives

W. Humphreys, Soong-Hoon Kim, R. Borzilleri, 2001 .

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.

Antroquinonol A: Scalable Synthesis and Preclinical Biology of a Phase 2 Drug Candidate

J. Fargnoli, R. Borzilleri, M. Fereshteh, 2015, ACS central science.

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

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.

DGKα/ζ inhibitors combine with PD-1 checkpoint therapy to promote T cell–mediated antitumor immunity

B. Cravatt, N. Meanwell, R. Borzilleri, 2023, Science Translational Medicine.

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

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

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 .