G. Vite

发表

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

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

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 BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.

S. Spergel, G. Trainor, L. Schweizer, 2015, ACS medicinal chemistry letters.

Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.

J. Chen, L. Schweizer, M. Salvati, 2010, Bioorganic & medicinal chemistry letters.

Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.

Michael A. Galella, A. Fura, S. Krystek, 2008, Bioorganic & medicinal chemistry letters.

Regioselective synthesis of folate receptor-targeted agents derived from epothilone analogs and folic acid.

Soong-Hoon Kim, F. Lee, H. Santhapuram, 2010, Bioorganic & medicinal chemistry letters.

Novel strategies for the discovery of plant-derived anticancer agents

G. Cordell, J. Pezzuto, C. Fairchild, 1994 .

Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations.

K. Nicolaou, D. Mandal, G. Vite, 2016, Journal of the American Chemical Society.

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.

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.

SAR and pH stability of cyano-substituted epothilones.

Soong-Hoon Kim, Kenneth J. Leavitt, C. Fairchild, 2002, Organic letters.

Synthesis, structure proof, and biological activity of epothilone cyclopropanes.

J. Tokarski, C. Fairchild, F. Lee, 2000, Organic letters.

The Discovery of BMS-737 as a Potent, CYP17 Lyase-Selective Inhibitor for the Treatment of Castration-Resistant Prostate Cancer.

J. Tokarski, A. Fura, L. Jayaraman, 2022, Bioorganic & medicinal chemistry letters.

Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.

A. Doweyko, G. Trainor, A. Fura, 2016, ACS medicinal chemistry letters.

Synergistic inhibition of A&bgr; production by combinations of &ggr;‐secretase modulators

M. Banks, M. Ahlijanian, D. Drexler, 2017, European journal of pharmacology.

Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Ping Chen, Derek J. Norris, J. Tokarski, 2011, Bioorganic & medicinal chemistry letters.

Silvestrol and episilvestrol, potential anticancer rocaglate derivatives from Aglaia silvestris.

G. Cordell, J. Pezzuto, A. Kinghorn, 2004, The Journal of organic chemistry.

Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity.

M. Barbacid, B. Seizinger, J. Hunt, 1996, Journal of medicinal chemistry.

Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads.

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

New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Henry Wong, Punit Marathe, John S Tokarski, 2007, Bioorganic & medicinal chemistry letters.

Pyrrolotriazine-5-carboxylate ester inhibitors of EGFR and HER2 protein tyrosine kinases and a novel one-pot synthesis of C-4 subsitituted pyrrole-2,3-dicarboxylate diesters

James G. Tarrant, B. Fink, T. Wong, 2006 .

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 anticancer agents of diverse natural origin

A. Kinghorn, D. Jarjoura, S. Emanuel, 2009, Pure and applied chemistry. Chimie pure et appliquee.

Identification of novel functional inhibitors of 17β‐hydroxysteroid dehydrogenase type III (17β‐HSD3)

I. Takenaka, B. Fink, M. Salvati, 2005 .

On the question of reversibility in the intramolecular addition of radicals to aldehydes to form cycloalkanols

G. Vite, B. A. Yeung, B. Fraser-Reid, 1988 .

Carbohydrates to carbocycles: synthesis of the densely functionalized carbocyclic core of tetrodotoxin by radical cyclization of an anhydro sugar precursor

G. Vite, R. Alonso, B. Fraser-Reid, 1993 .

Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer.

L. Schweizer, M. Salvati, Weifang Shan, 2009, Cancer research.

Generation of Oxygen-Centered Radicals by Reaction of Nitrate Esters with Tri-n-Butyltin Hydride

G. Vite, B. Fraser-Reid, 1988 .

Synthesis and biological activity of novel epothilone aziridines.

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

Radical cyclization routes to bridged pyranosides as precursors of densely functionalized cycloalkanes

R. Mcdevitt, G. Vite, R. Alonso, 1992 .

AlMe(3)-promoted formation of amides from acids and amines.

J. Kadow, J. Li, Jianqing Li, 2012, Organic letters.

Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.

J. Fargnoli, Derek J. Norris, J. Tokarski, 2009, Journal of medicinal chemistry.

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 .

Preparation d'intermediaires d'epothilone

Soong-Hoon Kim, G. Vite, G. Hoefle, 2001 .

Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.

Ping Chen, S. Spergel, O. Kocy, 1996, Journal of medicinal chemistry.

Intramolecular radical cyclizations of 2-deoxy-2-iodohexopyranoside derivatives: routes to densely functionalized carbocycles

G. Vite, R. Alonso, B. Fraser-Reid, 1989 .

Carbohydrates to Carbocycles via Radical Aldehyde Cyclizations

G. Vite, B. A. Yeung, R. Alonso, 1989 .

Generation of Oxygen-Centered Radicals by Reaction of Nitrate Esters with Tri-n-butyltin Hydride.

G. Vite, B. Fraser-Reid, 1989 .

Novel Reactions of Carbohydrates Discovered En Route to Natural Products

R. Mcdevitt, G. Vite, R. Alonso, 2010 .

Synthesis of (±)-7-epivaleranone and (±)-valeranone

G. Vite, T. A. Spencer, 1988 .

A Facile Method for the Transformation of N-(tert-Butoxycarbonyl) α-Amino Acids to N-Unprotected α-Amino Methyl Esters

O. Kocy, G. Vite, A. P. Skoumbourdis, 1999 .

Anticancer Agents: Frontiers in Cancer Chemotherapy

K. Altmann, I. Ojima, G. Vite, 2001 .

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.

Erratum: Silvestrol and episilvestrol, potential anticancer rocaglate derivatives from Aglaia silvestris (Journal of Organic Chemistry (2004) 69 (3350-3357))

G. Cordell, J. Pezzuto, A. Kinghorn, 2004 .

Silvestrol and episilvestrol, potential anticancer rocaglate derivatives from Aglaia silvestris.

G. Cordell, J. Pezzuto, A. Kinghorn, 2004, The Journal of organic chemistry.

Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.

J. Hunt, S. P. Seitz, K. Covello, 2017, Bioorganic & medicinal chemistry letters.

BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent.

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

Total Synthesis of Meayamycin and O-Acyl Analogues.

D. Boger, Anindya Sarkar, G. Vite, 2020, Organic letters.

A practical, efficient large-scale synthesis of 1,6-anhydrohexopyranoses

G. Vite, R. Alonso, B. Fraser-Reid, 1989 .

Differences in antiviral activities for isomers of a fluorinated cyclobutane nucleoside analog

G. Vite, J. Tino, R. Zahler, 1993 .

Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.

S. Chong, J. Hunt, Soong-Hoon Kim, 2000, Journal of medicinal chemistry.

α-hydroxyamide derived aminodiols as potent inhibitors of hiv protease

Ping Chen, S. Spergel, J. Barrish, 1995 .

Identification of novel functional inhibitors of 17beta-hydroxysteroid dehydrogenase type III (17beta-HSD3).

I. Takenaka, B. Fink, M. Salvati, 2005, The Prostate.

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

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

Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.

Derek J. Norris, J. Tokarski, S. D. Kimball, 2006, Bioorganic & medicinal chemistry letters.

Antitumor and Antiangiogenic Activities of BMS-690514, an Inhibitor of Human EGF and VEGF Receptor Kinase Families

J. Fargnoli, Derek J. Norris, J. Hunt, 2011, Clinical 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.

Preclinical Antitumor Activity of BMS-599626, a pan-HER Kinase Inhibitor That Inhibits HER1/HER2 Homodimer and Heterodimer Signaling

J. Hunt, F. Lee, B. Fink, 2006, Clinical Cancer Research.

[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.

Michael A. Galella, G. Trainor, Weifang Shan, 2016, Bioorganic & medicinal chemistry letters.

Hyperdynamic Microtubules, Cognitive Deficits, and Pathology Are Improved in Tau Transgenic Mice with Low Doses of the Microtubule-Stabilizing Agent BMS-241027

F. Lee, Soong-Hoon Kim, C. Janus, 2012, The Journal of Neuroscience.

Uncialamycin as a novel payload for antibody drug conjugate (ADC) based targeted cancer therapy.

D. Langley, Yichong Wang, P. Sivaprakasam, 2019, Bioorganic & medicinal chemistry letters.

Antibody-drug conjugates: current status and future directions.

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

Chemical Modification of Linkers Provides Stable Linker-Payloads for the Generation of Antibody-Drug Conjugates.

A. Mathur, H. D. King, G. Vite, 2020, ACS medicinal chemistry letters.

Design, synthesis and biological evaluation of phenol-linked uncialamycin antibody-drug conjugates.

A. Mathur, G. Vite, Y. Poudel, 2019, Bioorganic & medicinal chemistry letters.

New dual inhibitors of EGFR and HER2 protein tyrosine kinases.

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

Constitutively active receptor tyrosine kinases as oncogenes in preclinical models for cancer therapeutics

F. Lee, B. Fink, K. Kellar, 2006, Molecular Cancer Therapeutics.

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.

New Anticancer Drugs from Cultured and Collected Marine Organisms

Eric J. Kantorowski, Y. Shimizu, C. Fairchild, 2003 .

DNA-Model-Based Design and Execution of Some Fused Benzodiazepine Hybrid Payloads for Antibody-Drug Conjugate Modality.

Martin D. Eastgate, D. Langley, I. Mcdonald, 2021, ACS medicinal chemistry letters.

Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1

Alan S. Futran, S. Sheriff, B. Pearce, 2021, ACS medicinal chemistry letters.

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 .

Novel C-5 aminomethyl pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Henry Wong, Punit Marathe, John S Tokarski, 2007, Bioorganic & medicinal chemistry letters.

5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Henry Wong, Punit Marathe, John S Tokarski, 2007, Bioorganic & medicinal chemistry letters.

Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.

J. Hunt, V. Manne, C. Ricca, 1999, Journal of medicinal chemistry.

A Facile Method for the Transformation of N-(tert-Butoxycarbonyl) α-Amino Acids to N-Unprotected α-Amino Methyl Esters.

O. Kocy, G. Vite, P. Guo, 2000 .

Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.

J. Hunt, David K. Williams, Weifang Shan, 2018, Bioorganic & medicinal chemistry letters.

Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer.

L. Schweizer, M. Salvati, Weifang Shan, 2009, Cancer research.

Discovery of Non-Nucleotide Small-Molecule STING Agonists via Chemotype Hybridization.

Alan S. Futran, Vijay T. Ahuja, Shana L. Posy, 2022, Journal of medicinal chemistry.