T. Williams

发表

Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.

Christopher M Thomas, J. Hoffman, J. Wai, 1993, Journal of medicinal chemistry.

Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.

G. McGaughey, Youwei Yan, M. Lai, 2008, Journal of medicinal chemistry.

The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.

G. McGaughey, Youwei Yan, M. Lai, 2008, Bioorganic & medicinal chemistry letters.

Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.

G. McGaughey, Youwei Yan, M. Lai, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.

G. McGaughey, Youwei Yan, M. Lai, 2011, Journal of medicinal chemistry.

Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.

A. D. Rodrigues, E S Walsh, J B Gibbs, 2001, Journal of medicinal chemistry.

Farnesyltransferase inhibitors and anti-Ras therapy

N. Rosen, N. Kohl, L. Sepp-Lorenzino, 2005, Breast Cancer Research and Treatment.

P450 interaction with farnesyl-protein transferase inhibitors metabolic stability, inhibitory potency, and P450 binding spectra in human liver microsomes.

C. Tang, J. Lin, J. Wai, 2001, Biochemical pharmacology.

Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.

Kenneth D Anderson, M. Lai, J. Vacca, 2009, Journal of medicinal chemistry.

Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.

Kenneth D Anderson, M. Lai, J. Vacca, 2010, Bioorganic & medicinal chemistry letters.

Antiviral Activity of MK-4965, a Novel Nonnucleoside Reverse Transcriptase Inhibitor

D. Hazuda, Michael D. Miller, M. Lai, 2009, Antimicrobial Agents and Chemotherapy.

Inhibitors of protein farnesylation 1998

T. Williams, 1998 .

Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

J. Davide, R. Lobell, C. Buser, 2002, Bioorganic & medicinal chemistry letters.

Mechanism based neurotoxicity of mGlu5 positive allosteric modulators – Development challenges for a promising novel antipsychotic target

Sarah L. Huszar, J. Uslaner, T. Tucker, 2014, Neuropharmacology.

Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.

S. Stirdivant, L. Kuo, P. Darke, 2005, Biochemistry.

2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.

N. Kohl, R. Lobell, C. Buser, 2001, Bioorganic & medicinal chemistry letters.

An Improved Synthesis of Imidazo[4,5‐b]pyridines and Imidazo[4,5‐b]pyrazines by Palladium Catalyzed Amidation using Xantphos in a 1,4‐Dioxane:tert‐Amyl Alcohol Solvent System

Ijaz Ahmed, T. Williams, Adam J Rosenberg, 2014 .

Inhibitors of protein prenylation 1999

T. Williams, 1999 .

Identification of a novel RAMP-independent CGRP receptor antagonist.

J. Vacca, S. Graham, R. Z. Rutledge, 2011, Bioorganic & medicinal chemistry letters.

Pharmacological Characterization of MK-0974 [N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a Potent and Orally Active Calcitonin Gene-Related Peptide Receptor Antagonist for the Treatment of

A. W. Shaw, J. Vacca, Victor K. Johnston, 2008, Journal of Pharmacology and Experimental Therapeutics.

Active CGRP Receptor Antagonist for the Treatment of Migraine

A. W. Shaw, J. Vacca, S. Graham, 2007 .

Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.

J. Davide, N. Kohl, R. Lobell, 2001, Bioorganic & medicinal chemistry letters.

Preclinical Models Geranylgeranyl : Protein Transferase Inhibitor Combinations in Evaluation of Farnesyl : Protein Transferase and Updated

A. Kral, D. Heimbrook, J. Davide, 2001 .

Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.

T. Ciccarone, N. Kohl, J. Gibbs, 1999, Bioorganic & Medicinal Chemistry Letters.

Differential effects of the mGluR5 positive allosteric modulator CDPPB in the cortex and striatum following repeated administration

S. Doran, J. Uslaner, M. Jacobson, 2012, Neuropharmacology.

Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.

A. W. Shaw, S. Graham, R. Z. Rutledge, 2007, Bioorganic & medicinal chemistry letters.

Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.

J. Vacca, S. Graham, R. Z. Rutledge, 2006, Bioorganic & medicinal chemistry letters.

Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).

A. W. Shaw, J. Vacca, Victor K. Johnston, 2007, Journal of medicinal chemistry.

2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.

T. Ciccarone, A. Kral, J. Davide, 1996, Journal of medicinal chemistry.

Efficient synthesis of 1-heterocyclic-3-aminopyrrolidinones

T. Williams, I. M. Bell, S. N. Gallicchio, 2000 .

Synthesis of 2-amino-imidazo[4,5-b]pyridines.

T. Williams, Adam J Rosenberg, Daniel A. Clark, 2013, Organic & biomolecular chemistry.

Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.

A. W. Shaw, J. Vacca, H. Selnick, 2011, Bioorganic & medicinal chemistry letters.

Synthesis of the (3R,6S)-3-amino-6-(2,3-difluorophenyl)azepan-2-one of telcagepant (MK-0974), a calcitonin gene-related peptide receptor antagonist for the treatment of migraine headache.

A. W. Shaw, J. Vacca, S. Graham, 2008, Organic letters.

5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.

W. Greenlee, T. Ciccarone, J. Condra, 1993, Journal of medicinal chemistry.

Calcitonin gene-related peptide receptor antagonists for the treatment of migraine.

T. Williams, C. Salvatore, C. Burgey, 2009, Progress in medicinal chemistry.

Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.

Christopher M Thomas, W. S. Saari, J. Hoffman, 1993, Journal of medicinal chemistry.

Monophenolic 1,2,3,4-tetrahydroisoquinolines and their methyl

A. Brossi, T. Williams, R. A. Schmidt, 1971 .

Methyl 2,3-dideoxy-3-nitro-D-erythro-pentofuranoside, isomers and derivatives

H. Mosher, T. Williams, R. Nachman, 1986 .

Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).

G. McGaughey, Youwei Yan, L. Gabryelski, 2008, Bioorganic & medicinal chemistry letters.

5‐Chloro‐3‐(phenylsulfonyl)indole‐2‐carboxamide: A Novel, Non‐ Nucleoside Inhibitor of HIV‐1 Reverse Transcriptase.

W. Greenlee, P. Anderson, T. Ciccarone, 1994 .

Potent benzimidazolone-based CGRP receptor antagonists.

Cory R. Theberge, J. Vacca, Victor K. Johnston, 2008, Bioorganic & medicinal chemistry letters.

Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.

Cory R. Theberge, J. Vacca, J. Hochman, 2006, Bioorganic & medicinal chemistry letters.

The discovery of highly potent CGRP receptor antagonists.

Cory R. Theberge, J. Vacca, Victor K. Johnston, 2009, Bioorganic & medicinal chemistry letters.

dl-Isoserine and related compounds

H. Mosher, T. Williams, R. Crumbie, 1985 .

A chiral nitronate dianion from (=d)-glyceraldehyde. Enantiospecific syntheses of 2,3-dideoxy-3-nitro furanosides and pyranosides

H. Mosher, T. Williams, 1985 .

Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.

N. Kohl, R. Lobell, J. Gibbs, 1999, Bioorganic & medicinal chemistry letters.

Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.

J. Davide, N. Kohl, R. Lobell, 2001, Bioorganic & medicinal chemistry letters.

Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.

A. Kral, D. Heimbrook, J. Davide, 2001, Cancer research.

Patent Update Oncologic, Endocrine & Metabolic: Oncologic, Endocrine & Metabolic: Inhibitors of protein farnesylation

S. Graham, T. Williams, 1996 .

Isolation of macrocyclic trichothecenes from a large-scale extract of to Baccharis megapotamica

T. Williams, F. Boettner, B. Jarvis, 1987 .

3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.

A. D. Rodrigues, J Christopher Culberson, Ronald Robinson, 2002, Journal of medicinal chemistry.

Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

J. Davide, N. Kohl, R. Lobell, 2001, Bioorganic & medicinal chemistry letters.

Methyl 3-formyl-2,3-O-isopropylidene-D-erythrofuranoside (D-apiose aldal) and derivatives

H. Mosher, T. Williams, R. Nachman, 1986 .

Anions Modulate the Potency of Geranylgeranyl-Protein Transferase I Inhibitors*

D. Heimbrook, R. Lobell, C. Buser, 2001, The Journal of Biological Chemistry.

N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.

J. Huff, J. Davide, N. Kohl, 1999, Journal of medicinal chemistry.

Developing Small Molecules that Inhibit K-Ras/GTP Binding Based on New Affinity Measurements

M. Quick, M. Rudolph, C. Reynolds, 2020, bioRxiv.

Farnesyl transferase inhibitors: Design of a new class of cancer chemotherapeutic agents

T. Williams, C. Dinsmore, 1999 .

Distinct Mutation Pathways of Non-Subtype B HIV-1 during In Vitro Resistance Selection with Nonnucleoside Reverse Transcriptase Inhibitors

D. Hazuda, G. McGaughey, Youwei Yan, 2010, Antimicrobial Agents and Chemotherapy.

Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.

J. Vacca, P. Kunapuli, S. Graham, 2006, Bioorganic & medicinal chemistry letters.

The synthesis of substituted 2,3-dihydrothieno[2,3,b]-thiophenes via intramolecular Michael addition

K. Shepard, T. Williams, C. A. Hunt, 1991 .

The preparation of 5‐substituted thieno[2,3‐b]furan‐2‐sulfonamides

G. Hartman, T. Williams, J. D. Prugh, 1990 .

Antiviral Activity and In Vitro Mutation Development Pathways of MK-6186, a Novel Nonnucleoside Reverse Transcriptase Inhibitor

D. Hazuda, G. McGaughey, Youwei Yan, 2012, Antimicrobial Agents and Chemotherapy.

Mutational Analysis of Conserved Residues of the β-Subunit of Human Farnesyl:Protein Transferase*

R. Diehl, A. Kral, N. Kohl, 1997, The Journal of Biological Chemistry.

Comparison of imidazole- and 2-methyl imidazole-containing farnesyl-protein transferase inhibitors: interaction with and metabolism by rat hepatic cytochrome P450s.

J. Hochman, C. Tang, J. Lin, 2000, Drug metabolism and disposition: the biological fate of chemicals.

Attenuation of scratch‐induced reactive astrogliosis by novel EphA4 kinase inhibitors

Sujata Sharma, Hemaka A. Rajapakse, J. Vacca, 2011, Journal of neurochemistry.

Farnesyltransferase inhibitors: a new class of cancer chemotherapeutics.

N. Kohl, J. Gibbs, S. Graham, 1996, Biochemical Society transactions.

Conformational restriction of flexible ligands guided by the transferred noe experiment: potent macrocyclic inhibitors of farnesyltransferase.

J. Huff, M. Bogusky, S. Graham, 2001, Journal of the American Chemical Society.

Activation of the mGlu5 Receptor for the Treatment of Schizophrenia and Cognitive-Deficit-Associated Disorders

M. Jacobson, T. Williams, M. Kalinichev, 2014 .

Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants.

Kenneth D Anderson, Youwei Yan, M. Lai, 2009, Bioorganic & Medicinal Chemistry Letters.

Investigation of the species selectivity of a nonpeptide CGRP receptor antagonist using a novel pharmacodynamic assay

R. Hargreaves, T. Williams, E. Baskin, 2005, Regulatory Peptides.

Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth

A. Burkhardt, N. Kohl, R. Lobell, 1997, BioFactors.

Identification of potent, highly constrained CGRP receptor antagonists.

Steven S. Sharik, Cory R. Theberge, J. Vacca, 2010, Bioorganic & medicinal chemistry letters.

The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.

Cory R. Theberge, J. Vacca, Victor K. Johnston, 2009, Bioorganic & medicinal chemistry letters.

Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.

J. Vacca, T. Williams, Sean Yu, 2009, Bioorganic & medicinal chemistry letters.