K. Santone

发表

Drug Metabolism in Drug Development: A DIA Tutorial for Regulatory Affairs Specialists*

L. Cantilena, P. Honig, K. Santone, 1998 .

Anthracycline-induced inhibition of a calcium action potential in differentiated murine neuroblastoma cells.

G. Powis, K. Santone, S. Oakes, 1986, Cancer research.

Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity.

B. Beno, N. Meanwell, Zeyu Lin, 2016, ACS medicinal chemistry letters.

Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.

L. Hamann, A. Fura, N. Meanwell, 2014, Journal of medicinal chemistry.

An automated high throughput liquid chromatography-mass spectrometry process to assess the metabolic stability of drug candidates.

James V Belcastro, K. Dickinson, C. Mcnaney, 2007, Assay and drug development technologies.

Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators.

M. D. Hill, J. Macor, T. Molski, 2016, ACS medicinal chemistry letters.

Quinoneimines as substrates for quinone reductase (NAD(P)H: (quinone-acceptor)oxidoreductase) and the effect of dicumarol on their cytotoxicity.

G. Powis, K. Santone, D. Melder, 1987, Biochemical pharmacology.

A high-performance liquid chromatography assay for measuring integrated biphenyl metabolism by intact cells: its use with rat liver and human liver and kidney.

G. Powis, T. Wilke, K. Santone, 1987, Analytical biochemistry.

Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.

J. Macor, R. Schartman, G. Tong, 2012, Journal of medicinal chemistry.

Cryopreservation of rat and dog hepatocytes for studies of xenobiotic metabolism and activation.

G. Powis, T. Wilke, K. Santone, 1987, Drug metabolism and disposition: the biological fate of chemicals.

An in vitro approach to the study of target organ toxicity of drugs and chemicals

D. Acosta, K. Ramos, E. M. Sorensen, 1985, In Vitro Cellular & Developmental Biology.

Involvement of cytochrome P‐450 isozymes in melatonin metabolism and clinical implications

K. Santone, N. Vachharajani, K. Yeleswaram, 1999, Journal of pineal research.

Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.

A. Good, H. Klei, A. Cocuzza, 2014, Journal of medicinal chemistry.

Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents.

N. Meanwell, P. Shi, K. Yeung, 2013, Bioorganic & medicinal chemistry letters.

Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.

Chong-Hwan Chang, M. Witmer, B. Beno, 2014, Journal of medicinal chemistry.

Biaryl isoxazolinone antibacterial agents.

Dennis K. Taylor, G. Warr, A. Marinier, 2005, Bioorganic & medicinal chemistry letters.

Studies of chemical toxicity to fresh and cryopreserved rat hepatocytes.

G. Powis, K. Santone, D. Melder, 1989, Toxicology and applied pharmacology.

Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.

J. Macor, Amy Easton, Anand Balakrishnan, 2016, ACS medicinal chemistry letters.

Evaluation of cytotoxicity in cultured cells by enzyme leakage

D. Acosta, K. Santone, D. Mitchell, 1980 .

Effects of advanced leukemia on hepatic drug-metabolizing activity in the mouse

G. Powis, P. Basseches, K. Santone, 2004, Cancer Chemotherapy and Pharmacology.

Measurement of functional metabolic activity as a sensitive parameter of cytotoxicity in cultured hepatocytes

D. Acosta, K. Santone, 1982 .

Cadmium toxicity in primary cultures of rat hepatocytes.

D. Acosta, J. Bruckner, K. Santone, 1982, Journal of toxicology and environmental health.

Lack of cytotoxicity of ticrynafen in primary cultures of rat liver cells.

D. Acosta, W. Lewis, K. Santone, 1982, Toxicology letters.

Role of metabolism and oxidation-reduction cycling in the cytotoxicity of antitumor quinoneimines and quinonediimines.

G. Powis, K. Santone, D. Melder, 1987, Cancer research.

Preclinical Characterization of BMS-791325, an Allosteric Inhibitor of Hepatitis C Virus NS5B Polymerase

N. Meanwell, J. Lemm, R. Colonno, 2014, Antimicrobial Agents and Chemotherapy.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain

Alan G. E. Wilson, G. Shankar, S. Mandlekar, 2016, The Journal of Pharmacology and Experimental Therapeutics.

Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.

J. Macor, Amy Easton, Anand Balakrishnan, 2016, Bioorganic & medicinal chemistry letters.

Structure-Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors.

M. Witmer, B. Beno, K. Kish, 2018, ACS medicinal chemistry letters.

Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.

Qi Gao, Min Gao, Steven Sheriff, 2017, Journal of medicinal chemistry.

Preclinical Pharmacokinetics and In Vitro Metabolism of Asunaprevir (BMS-650032), a Potent Hepatitis C Virus NS3 Protease Inhibitor.

Y. Shu, V. Arora, Anand Balakrishnan, 2015, Journal of pharmaceutical sciences.

An increase in intracellular free Ca2+ associated with serum-free growth stimulation of Swiss 3T3 fibroblasts by epidermal growth factor in the presence of bradykinin.

G. Powis, R. Abraham, R. Olsen, 1988, The Journal of biological chemistry.

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.

G. Shankar, J. Macor, C. Albright, 2022, Journal of medicinal chemistry.

Discovery of (S)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.

Alan G. E. Wilson, G. Shankar, J. Macor, 2022, Journal of medicinal chemistry.

Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,1

B. Beno, N. Meanwell, V. Arora, 2018, Journal of medicinal chemistry.

Enhanced formation of ethane and n-pentane by rat hepatocytes in the presence of dimethyl sulfoxide.

G. Powis, K. Santone, D. M. Kroschel, 1986, Biochemical pharmacology.

Design and Characterization of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transporter Activity

J. Polli, J. Raufman, Su Xu, 2013, Pharmaceutical Research.

Role of regional absorption and gastrointestinal motility on variability in oral absorption of a model drug

A. Narang, Anand Balakrishnan, Jennifer J Wang, 2017, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

Preclinical pharmacokinetics and in vitro metabolism of BMS-605339: a novel HCV NS3 protease inhibitor.

V. Arora, J. Knipe, F. Mcphee, 2014, Journal of pharmaceutical sciences.

Preclinical pharmacokinetics of a novel HIV‐1 attachment inhibitor BMS‐378806 and prediction of its human pharmacokinetics

A. Marino, N. Meanwell, R. Colonno, 2005, Biopharmaceutics & drug disposition.

Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain

A. Good, J. Macor, L. Bristow, 2023, Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents.

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.

J. Macor, Amy Easton, Anand Balakrishnan, 2016, Bioorganic & medicinal chemistry letters.

The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.

A. Mathur, N. Meanwell, Zeyu Lin, 2022, Journal of medicinal chemistry.

Effect of some anticancer drugs on the surface membrane electrical properties of differentiated murine neuroblastoma cells.

G. Powis, K. Santone, S. Oakes, 1987, Journal of the National Cancer Institute.

Inhibition of AAK 1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain s

Alan G. E. Wilson, Malley, G. Shankar, 2016 .

Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes.

V. Gribkoff, R. Dalterio, C. Boissard, 2005, Bioorganic & Medicinal Chemistry Letters.

Analogues (Ib)‐(Ic) of a Potent Maxi‐K Potassium Channel Opener (Ia) with an Improved Inhibitory Profile Toward Cytochrome P450 Isozymes.

V. Gribkoff, R. Dalterio, C. Boissard, 2005 .

Studies on the pharmacokinetics and metabolism of a γ-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction

J. Lubinski, O. Flint, D. Boulton, 2009, Xenobiotica; the fate of foreign compounds in biological systems.

Inhibitors of HIV-1 attachment. Part 8: the effect of C7-heteroaryl substitution on the potency, and in vitro and in vivo profiles of indole-based inhibitors.

T. Spicer, N. Meanwell, P. Shi, 2013, Bioorganic & medicinal chemistry letters.

Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.

A. Good, H. Klei, A. Cocuzza, 2014, Journal of medicinal chemistry.